Page last updated: 2024-11-05

nimorazole

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Nimorazole: An antitrichomonal agent which is effective either topically or orally and whose urinary metabolites are also trichomonicidal. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23009
CHEMBL ID435966
CHEBI ID134929
SCHEMBL ID21836
MeSH IDM0014861
PubMed CID49864510
CHEMBL ID1221986
MeSH IDM0014861

Synonyms (76)

Synonym
smr001570693
nimorazol [inn-spanish]
morpholine, 4-(2-(5-nitroimidazol-1-yl)ethyl)-
1-(n-p-ethylmorpholine)-5-nitroimidazole
einecs 229-394-4
4-(2-(5-nitroimidazol-1-yl)ethyl)morpholine
brn 0533758
sirledi
nimorazolo [dcit]
k 1900
4-(2-(5-nitroimidazol-1-yl)ethyl)-morpholine
morpholine, 4-(2-(5-nitro-1h-imidazol-1-yl)ethyl)-
nsc 107524
nimorazolum [inn-latin]
1-(beta-morpholinoethyl)-5-nitroimidazole
naxogin (tn)
nimorazole (inn)
D07352
mls002703984 ,
k-1900 ,
nsc-107524
nitrimidazine
4-[2-(5-nitroimidazol-1-yl)ethyl]morpholine
nulogyl
morpholine, 4-[2-(5-nitroimidazol-1-yl)ethyl]-
nimorazol
1-(2-n-morpholinylethyl)-5-nitroimidazole
n-2-morpholinoethyl-5-nitroimidazole
acterol forte
acterol
esclama
6506-37-2
nsc107524
1-(.beta.-morpholinoethyl)-5-nitroimidazole
wln: t6n dotj a2- at5n cnj enw
naxofem
nimorazole
naxogin
morpholine, 4-[2-(5-nitro-1h-imidazol-1-yl)ethyl]-
CHEBI:134929
CHEMBL435966
A834961
nimorazolo
nimorazolum
nimorazole [inn:ban]
unii-469ulx0h4g
469ulx0h4g ,
S6411
nimorazole [mart.]
nimorazole [mi]
nimorazole [who-dd]
nimorazole [inn]
HY-16349
AKOS022174968
AM807557
4-(2-(5-nitro-1h-imidazol-1-yl)ethyl)morpholine
SCHEMBL21836
dtxsid1057795 ,
NCGC00261977-01
cas-6506-37-2
tox21_113897
dtxcid2031584
MDJFHRLTPRPZLY-UHFFFAOYSA-N
4-[2-(5-nitro-1h-imidazol-1-yl)ethyl]morpholine #
AC-35227
4-[2-(5-nitro-1h-imidazol-1-yl)ethyl]morpholine
mfcd00866796
DB12172
FT-0710009
AS-31120
BCP11055
Q7037737
A13091
CHEMBL1221986
nsc-101088
DBRXOUCRJQVYJQ-BZMBVROXSA-N

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"To study the pharmacokinetic characteristics of the hypoxic radiosensitiser nimorazole in patients with head and neck squamous cell carcinoma."( Study of the population pharmacokinetic characteristics of nimorazole in head and neck cancer patients treated in the DAHANCA-5 trial.
Hassan Metwally, MA; Jansen, JA; Overgaard, J, 2015
)
0.89
" Plasma concentration profiles were subjected to non-compartmental pharmacokinetic analysis using validated PC-based software."( Study of the population pharmacokinetic characteristics of nimorazole in head and neck cancer patients treated in the DAHANCA-5 trial.
Hassan Metwally, MA; Jansen, JA; Overgaard, J, 2015
)
0.66
" The mean peak concentration adjusted for dose (in g/m(2)) was 32."( Study of the population pharmacokinetic characteristics of nimorazole in head and neck cancer patients treated in the DAHANCA-5 trial.
Hassan Metwally, MA; Jansen, JA; Overgaard, J, 2015
)
0.66
" The LC-MS/MS method described here was validated and successfully applied to pharmacokinetic study in rats."( A rapid and sensitive determination of hypoxic radiosensitizer agent nimorazole in rat plasma by LC-MS/MS and its application to a pharmacokinetic study.
Bal, T; Das, S; Dubey, R; Ghosh, M; Kumar Pradhan, K; Muthukrishnan, V; Pujarid, A; Roychowdhury, S; Seijas, JA; Sinha, BN, 2015
)
0.65

Compound-Compound Interactions

Nimorazole combined with RCTx improved local tumor control in some but not in all HNSCC xenografts. It is unknown whether this holds also for radiochemotherapy (RCTx)

ExcerptReferenceRelevance
" In head and neck squamous cell carcinoma (HNSCC), nimorazole, an oxygen mimic, combined with radiotherapy (RT) enabled to improve loco-regional control (LRC) in some patients with hypoxic tumors but it is unknown whether this holds also for radiochemotherapy (RCTx)."( Prognostic biomarkers for the response to the radiosensitizer nimorazole combined with RCTx: a pre-clinical trial in HNSCC xenografts.
Baumann, M; Besso, MJ; Bitto, V; Koi, L; Krause, M; Kurth, I; Linge, A; Löck, S; Möbius, L; Overgaard, J; Pfeifer, M; Valentini, C; Weise, C; Yaromina, A; Zips, D, 2023
)
1.4
"Irradiations were performed with 30 fractions in 6 weeks combined with weekly cisplatin."( Prognostic biomarkers for the response to the radiosensitizer nimorazole combined with RCTx: a pre-clinical trial in HNSCC xenografts.
Baumann, M; Besso, MJ; Bitto, V; Koi, L; Krause, M; Kurth, I; Linge, A; Löck, S; Möbius, L; Overgaard, J; Pfeifer, M; Valentini, C; Weise, C; Yaromina, A; Zips, D, 2023
)
1.15
"Nimorazole combined with RCTx significantly improved permanent local control in two tumor models, and showed a potential improvement in two additional models."( Prognostic biomarkers for the response to the radiosensitizer nimorazole combined with RCTx: a pre-clinical trial in HNSCC xenografts.
Baumann, M; Besso, MJ; Bitto, V; Koi, L; Krause, M; Kurth, I; Linge, A; Löck, S; Möbius, L; Overgaard, J; Pfeifer, M; Valentini, C; Weise, C; Yaromina, A; Zips, D, 2023
)
2.59
"Nimorazole combined with RCTx improved local tumor control in some but not in all HNSCC xenografts."( Prognostic biomarkers for the response to the radiosensitizer nimorazole combined with RCTx: a pre-clinical trial in HNSCC xenografts.
Baumann, M; Besso, MJ; Bitto, V; Koi, L; Krause, M; Kurth, I; Linge, A; Löck, S; Möbius, L; Overgaard, J; Pfeifer, M; Valentini, C; Weise, C; Yaromina, A; Zips, D, 2023
)
2.59

Dosage Studied

The effectiveness of metronidazole and nimorazole (Naxogin) has been compared by using these drugs in the recommended dosage in alternate patients in a series of 218 cases of vaginal trichomoniasis.

ExcerptRelevanceReference
"The effectiveness of metronidazole (Flagyl) and nimorazole (Naxogin) has been compared by using these drugs in the recommended dosage in alternate patients in a series of 218 consecutive cases of vaginal trichomoniasis."( Treatment of trichomoniasis in the female. A comparison of metronidazole and nimorazole.
Heasman, L; Laird, SM; Roy, RB, 1975
)
0.74
" This dosage consistently yielded plasma concentrations above 30 microg/ml."( Treatment of head and neck cancer with CHART and nimorazole: phase II study.
Bishop, K; Henk, JM; Shepherd, SF, 2003
)
0.57
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
imidazolesA five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
C-nitro compoundA nitro compound having the nitro group (-NO2) attached to a carbon atom.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency2.11320.006038.004119,952.5996AID1159521
TDP1 proteinHomo sapiens (human)Potency29.09290.000811.382244.6684AID686978
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency33.49150.001022.650876.6163AID1224838
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
Guanine nucleotide-binding protein GHomo sapiens (human)Potency11.22021.995325.532750.1187AID624287
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAC-alpha serine/threonine-protein kinaseHomo sapiens (human)Activity2.50002.50002.50002.5000AID504164
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (139)

Processvia Protein(s)Taxonomy
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
protein phosphorylationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
activation-induced cell death of T cellsRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
intracellular signal transductionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
osteoblast differentiationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
maternal placenta developmentRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of protein phosphorylationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of endothelial cell proliferationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cell migration involved in sprouting angiogenesisRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwayRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
glycogen biosynthetic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
regulation of glycogen biosynthetic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
glucose metabolic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
regulation of translationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein phosphorylationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of protein kinase activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein import into nucleusRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
nitric oxide biosynthetic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
inflammatory responseRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
response to oxidative stressRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
signal transductionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
epidermal growth factor receptor signaling pathwayRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
G protein-coupled receptor signaling pathwayRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
canonical NF-kappaB signal transductionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cell population proliferationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
insulin receptor signaling pathwayRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
apoptotic mitochondrial changesRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
response to heatRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
gene expressionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of autophagyRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of endothelial cell migrationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of gene expressionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of gene expressionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of long-chain fatty acid import across plasma membraneRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
fibroblast migrationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of fibroblast migrationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of sodium ion transportRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of glucose metabolic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of endopeptidase activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
regulation of neuron projection developmentRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of macroautophagyRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
phosphorylationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein ubiquitinationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
peptidyl-serine phosphorylationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
peptidyl-threonine phosphorylationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
virus-mediated perturbation of host defense responseRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cytokine-mediated signaling pathwayRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
mammalian oogenesis stageRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cell differentiationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of cell growthRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
regulation of cell migrationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of cell migrationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
T cell costimulationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of protein ubiquitinationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
regulation of myelinationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
lipopolysaccharide-mediated signaling pathwayRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
TOR signalingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of fatty acid beta-oxidationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of endodeoxyribonuclease activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of protein bindingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
response to foodRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
peripheral nervous system myelin maintenanceRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to insulin stimulusRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
response to fluid shear stressRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to reactive oxygen speciesRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
interleukin-18-mediated signaling pathwayRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to vascular endothelial growth factor stimulusRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to decreased oxygen levelsRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
non-canonical NF-kappaB signal transductionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
glucose homeostasisRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
regulation of apoptotic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of apoptotic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
anoikisRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
regulation of mRNA stabilityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of nitric oxide biosynthetic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of fat cell differentiationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of glycogen biosynthetic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of Notch signaling pathwayRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of proteolysisRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of DNA-templated transcriptionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of glucose importRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of organ growthRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein autophosphorylationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of lipid biosynthetic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
behavioral response to painRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of smooth muscle cell proliferationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of nitric-oxide synthase activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
striated muscle cell differentiationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of protein metabolic processRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
excitatory postsynaptic potentialRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
response to growth hormoneRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
mammary gland epithelial cell differentiationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
labyrinthine layer blood vessel developmentRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
response to UV-ARAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
response to growth factorRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to cadmium ionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to tumor necrosis factorRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to epidermal growth factor stimulusRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to prostaglandin E stimulusRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of protein serine/threonine kinase activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
establishment of protein localization to mitochondrionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
maintenance of protein location in mitochondrionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of release of cytochrome c from mitochondriaRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to granulocyte macrophage colony-stimulating factor stimulusRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
execution phase of apoptosisRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
regulation of postsynapse organizationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
regulation of tRNA methylationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to oxidised low-density lipoprotein particle stimulusRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of protein localization to lysosomeRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of cGAS/STING signaling pathwayRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of protein localization to nucleusRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to peptideRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
regulation of signal transduction by p53 class mediatorRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of cilium assemblyRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of oxidative stress-induced intrinsic apoptotic signaling pathwayRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of leukocyte cell-cell adhesionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of protein localization to plasma membraneRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of I-kappaB phosphorylationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of TORC1 signalingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of protein localization to endoplasmic reticulumRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cellular response to nerve growth factor stimulusRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
response to insulin-like growth factor stimulusRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
positive regulation of protein localization to cell surfaceRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
regulation of type B pancreatic cell developmentRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of lymphocyte migrationRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
intracellular signal transductionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
protein kinase activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein serine/threonine kinase activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein serine/threonine/tyrosine kinase activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein bindingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
calmodulin bindingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
ATP bindingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
phosphatidylinositol-3,4,5-trisphosphate bindingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
kinase activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
enzyme bindingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein kinase bindingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
nitric-oxide synthase regulator activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein serine/threonine kinase inhibitor activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
identical protein bindingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein homodimerization activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
phosphatidylinositol-3,4-bisphosphate bindingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
14-3-3 protein bindingRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
potassium channel activator activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein serine kinase activityRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
cytoplasmRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
mitochondrial intermembrane spaceRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
membraneRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
nucleusRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
nucleoplasmRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cytoplasmRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
spindleRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cytosolRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
plasma membraneRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cell-cell junctionRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
cell cortexRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
microtubule cytoskeletonRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
lamellipodiumRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
vesicleRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
ciliary basal bodyRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
postsynapseRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
glutamatergic synapseRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
protein-containing complexRAC-alpha serine/threonine-protein kinaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (278)

Assay IDTitleYearJournalArticle
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1454801Hypoxia radiosensitization activity in human HCT116 cells assessed as survival ratio by measuring ratio of cell survival with 15 Gy radiation in absence to presence of compound at anoxic IC50 preincubated for 1 hr followed by 15 Gy irradiation measured af2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1146193Antimicrobial activity against Staphylococcus aureus Tour by microtitre method1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Synthesis and biological activity of new 2-nitroimidazole derivatives.
AID84679Lowest active dose which cured hamsters with Entamoeba histolytica hepatic infection was measured1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Antiamebic amidines and sulfonamides of 5- and 6-amino-2,3-bis(4-alkyl-1-piperazinyl)quinoxalines.
AID23681Partition coefficient (logP)1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID194143The total 18 hr urinary excretion of unchanged compound reported as log (percent X 10) of the administered dose1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID1454875Cmax in tumor of NIH-III mouse xenografted with human HCT116 cells at 1.24 mmol/kg, iv administered as single dose by HPLC analysis2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1146200Acute toxicity in po dosed mouse1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Synthesis and biological activity of new 2-nitroimidazole derivatives.
AID1454887Cytotoxicity against human HCT116 cells at anoxic IC50 incubated for 1 hr at 21 degC by sulforhodamine B assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID16040Percent biliary excretion property by administering intravenously to rats was reported as amount of unchanged form of compound detected in bile samples collected at 0-5 hr after the treatment.1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
The influence of physicochemical parameters on the biliary excretion of a series of nitroimidazoles.
AID172617The amount of the unchanged form of compound detected in the urine samples collected at 0-18 hr after the treatment by HPLC technique; No data1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID173917Lowest active dose which cured rats with Entamoeba histolytica cecal infection was measured1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Antiamebic amidines and sulfonamides of 5- and 6-amino-2,3-bis(4-alkyl-1-piperazinyl)quinoxalines.
AID194145The total 54 h urinary excretion of unchanged compound reported as log (percent X 10) of the administered dose1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID1454815Hypoxia radiosensitization activity in human HCT116 cells assessed as sensitizer enhancement ratio by measuring ratio of radiation dose for 1% survival in absence to presence of compound at 9.8 mM preincubated for 1 hr followed by irradiation measured aft2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1146194Antimicrobial activity against Streptococcus pyogenes C 203 by microtitre method1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Synthesis and biological activity of new 2-nitroimidazole derivatives.
AID16038Percent biliary excretion property by administering intravenously to rats was reported as amount of unchanged form of compound detected in bile samples collected at 0-3 hr after the treatment.1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
The influence of physicochemical parameters on the biliary excretion of a series of nitroimidazoles.
AID16041Percent biliary excretion property by administering intravenously to rats was reported as amount of unchanged form of compound detected in bile samples collected at 0-6 hr after the treatment.1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
The influence of physicochemical parameters on the biliary excretion of a series of nitroimidazoles.
AID194144The total 36 hr urinary excretion of unchanged compound reported as log (percent X 10) of the administered dose1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID1454864Toxicity in NIH-III mouse at 10 ml/kg, iv2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1135605Antimicrobial activity against Entamoeba histolytica NIH 200-mu hepatic forms infected in golden hamster assessed as survival rate administered qd for 5 days measured up to 14 days by microscopic analysis1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Bisamidines of 2,6-diaminoanthraquinone as antiamebic agents.
AID172622The amount of unchanged compound in urine collected at 0-72 h after treatment1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID194142The total 18 hr urinary excretion of the unchanged form of compound in urine was reported as log (percent X 10) of the administered dose by HPLC technique; No data1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID1146199Antimicrobial activity against Trichomonas vaginalis infected in po dosed mouse relative to metronidazole1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Synthesis and biological activity of new 2-nitroimidazole derivatives.
AID1454797Solubility of the compound in alphaMEM containing 5% FCS and 1% DMSO by HPLC analysis2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID16036Percent biliary excretion property by administering intravenously to rats was reported as amount of unchanged form of compound detected in bile samples collected at 0-1 hr after the treatment.1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
The influence of physicochemical parameters on the biliary excretion of a series of nitroimidazoles.
AID1454883In vivo hypoxia radiosensitization activity in human HCT116 cells xenografted in NIH-III mouse assessed as survival ratio by measuring ratio of cell survival with 12.5 Gy radiation in absence to presence of compound at 1.24 mmol/kg, iv pretreated as singl2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1146195Antimicrobial activity against Clostridium perfringens ISS 30543 by broth dilution method1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Synthesis and biological activity of new 2-nitroimidazole derivatives.
AID172618The amount of unchanged compound detected in urine collected at 0-18 hr after treatment1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID1454846Hypoxia radiosensitization activity in human HCT116 cells assessed as survival ratio by measuring ratio of cell survival with radiation in absence to presence of compound at 9.8 mM preincubated for 1 hr followed by 6 to 29 Gy irradiation measured after 102018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1146198Antimicrobial activity against Trichomonas vaginalis infected in po dosed mouse1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Synthesis and biological activity of new 2-nitroimidazole derivatives.
AID23240Partition coefficient (logP)1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
The influence of physicochemical parameters on the biliary excretion of a series of nitroimidazoles.
AID1146197Antimicrobial activity against Trichomonas vaginalis by broth dilution method1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Synthesis and biological activity of new 2-nitroimidazole derivatives.
AID172621The amount of unchanged compound in urine collected at 0-54 hr after treatment1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID26535Capacity factor (log k')1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID1454828Hypoxia radiosensitization activity in human HCT116 cells assessed as survival ratio by measuring ratio of cell survival with radiation in absence to presence of compound at 9.8 mM preincubated for 1 hr followed by 6 to 29 Gy irradiation measured after 102018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1135604Antimicrobial activity against Entamoeba histolytica NIH 200-mu cecal forms infected in Wistar albino rat assessed as cure rate administered qd for 5 days by microscopic analysis1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Bisamidines of 2,6-diaminoanthraquinone as antiamebic agents.
AID16039Percent biliary excretion property by administering intravenously to rats was reported as amount of unchanged form of compound detected in bile samples collected at 0-4 hr after the treatment.1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
The influence of physicochemical parameters on the biliary excretion of a series of nitroimidazoles.
AID1454799Hypoxic cytotoxicity ratio of IC50 for human HCT116 cells under oxic condition to IC50 for human HCT116 cells under anoxic condition2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1454888Electrophilicity of the compound in pH 7 phosphate buffer assessed as one-electron reduction potential2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1454863Toxicity in NIH-III mouse xenografted with human HCT116 cells assessed as change in body weight with 15 Gy radiation at 0.93 mmol/kg, iv administered as single dose2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID194146The total 72 hr urinary excretion of unchanged compound reported as log (percent X 10) of the administered dose1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID1454798Cytotoxicity against human HCT116 cells incubated for 4 hrs under anaerobic condition measured after 5 days by sulforhodamine B assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1146196Antimicrobial activity against Mycoplasma gallisepticum S6 Weybridge by broth dilution method1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Synthesis and biological activity of new 2-nitroimidazole derivatives.
AID172620The amount of unchanged compound in urine collected at 0-36 hr after treatment1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Relationship between lipophilic character and urinary excretion of nitroimidazoles and nitrothiazoles in rats.
AID16037Percent biliary excretion property by administering intravenously to rats was reported as amount of unchanged form of compound detected in bile samples collected at 0-2 hr after the treatment.1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
The influence of physicochemical parameters on the biliary excretion of a series of nitroimidazoles.
AID1454879Tmax in tumor of NIH-III mouse xenografted with human HCT116 cells at 1.24 mmol/kg, iv administered as single dose by HPLC analysis2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1454867Cmax in plasma of NIH-III mouse xenografted with human HCT116 cells at 1.24 mmol/kg, iv administered as single dose by HPLC analysis2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1454802Hypoxia radiosensitization activity in human HCT116 cells assessed as sensitizer enhancement ratio by measuring ratio of radiation dose for 1% survival in absence to presence of compound at 9.8 mM preincubated for 1 hr followed by irradiation measured aft2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1146201Therapeutic index, ratio of LD50 for po dosed mouse to ED50 for Trichomonas vaginalis infected in po dosed mouse1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Synthesis and biological activity of new 2-nitroimidazole derivatives.
AID1454871Tmax in plasma of NIH-III mouse xenografted with human HCT116 cells at 1.24 mmol/kg, iv administered as single dose by HPLC analysis2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1240124Cytotoxicity against human DU145 cells after 24 hrs by FMCA2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Hedgehog inhibitors from Withania somnifera.
AID1240133Inhibition of GST-GLI1 (unknown origin) interaction with DNA assessed as reduction of protein-DNA complex level at 100 uM after 20 mins by electrophoretic mobility shift assay2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Hedgehog inhibitors from Withania somnifera.
AID774168Reduction in CHK1 phosphorylation at Ser345 in human PC3 cells at IC50 after 12 to 48 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID670613Induction of apoptosis in human HeLa cells assessed as DNA fragmentation at 16 to 32 uM after 24 hrs by agarose gel electrophoresis2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID504136Cytotoxicity against human JHU011 cells after 72 hrs by MTS assay2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID670625Induction of caspase 3 activation in human HeLa cells using Ac-DEVD-pNA at 24 uM after 8 hrs by Bradford assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID1256766Cytotoxicity against human MDA-MB-231 cells by MTT assay2015Journal of natural products, Oct-23, Volume: 78, Issue:10
Withanolides and Sucrose Esters from Physalis neomexicana.
AID774170Downregulation of Myt-1 protein expression in human PC3 cells at 1 uM after 12 to 48 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID774175Downregulation of cyclin E2 protein expression in human PC3 cells at IC50 after 12 to 48 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID774181Growth inhibition of human PC3 cells assessed as loss of cell viability after 24 hrs by trypan blue exclusion assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID502903Displacement of biotinyl-withaferin from bovine lung annexin 4 at 10 uM by chemiluminescence assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID774173Downregulation of cyclin B1 protein expression in human PC3 cells at IC50 after 12 to 48 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID360406Induction of IKK-beta-mediated IkappaBalpha degradation in IFN-stimulated mouse L929sA cells at 2.8 ug/ml by Western blot2007The Journal of biological chemistry, Feb-16, Volume: 282, Issue:7
Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity.
AID1130020Induction of heat shock protein-mediated heat shock response in mouse 3T3-Y9-B12 cells assessed as heat shock index after 24 hrs by fluorescence assay relative to control2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Structure-activity relationships for withanolides as inducers of the cellular heat-shock response.
AID360408Inhibition of TNF-induced NF-kappaB-mediated IL6 promoter expression in mouse L929sA cells by luciferase reporter gene assay2007The Journal of biological chemistry, Feb-16, Volume: 282, Issue:7
Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity.
AID504166Inhibition of Akt in human JMAR cells assessed as decrease in total protein level at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID1056312Cytotoxicity against human SK-MEL-28 cells after 72 hrs by MTS assay2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Synthesis and Cytotoxicity of Semisynthetic Withalongolide A Analogues.
AID504177Induction of apoptosis in human MDA1986 cells assessed as increase in early apoptotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID502909Induction of annexin 2-mediated F-actin disruption in human HepG2 cells at 4 uM after 2 hrs by confocal laser scanning microscopy2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID670610Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for human MCF7 cells after 48 hrs2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID502906Inhibition of annexin 2-mediated liposome aggregation after 15 mins by spectrophotometry2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID1130022Induction of heat shock activity in mouse assessed as upregulation of HSP72 protein level in spleen at 25 mg/kg, sc after 18 hrs by immunoblotting analysis2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Structure-activity relationships for withanolides as inducers of the cellular heat-shock response.
AID504152Induction of apoptosis in human JHU011 cells assessed as decrease in procaspase-3 level at 1 to 6 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID774178Induction of cell cycle arrest in human PC3 cells assessed as accumulation at G2/M phase at 1 uM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 25.3%)2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID774161Mitotic arrest in human PC3 cells assessed as punctate distribution of Aurora B in centromeric region of chromosomes by DAPI staining-based confocal microscopic analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID1241665Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell proliferation/survival after 72 hrs by resazurin dye reduction assay2015Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
Discovery of Potent 17β-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.
AID502901Displacement of biotinyl-withaferin from bovine lung annexin 2 at 10 uM by chemiluminescence assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID502913Cytotoxicity against human WI38 cells assessed as cell viability pretreated after 16 hrs by MTT assay in presence of 1 uM cytochalasin B2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID639260Cytotoxicity against human MDA1986 cells after 72 hrs by MTS assay2011Journal of natural products, Dec-27, Volume: 74, Issue:12
Cytotoxic withanolide constituents of Physalis longifolia.
AID502919Effect on human F-actin pellet formation after 1 hr by SDS-PAGE2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID286448Cytotoxicity against human Hep3B cells by MTT method2007Journal of natural products, May, Volume: 70, Issue:5
Cytotoxic withanolides from Tubocapsicum anomalum.
AID502918Effect on human F-actin bundling assessed as light scattering after 1 hr by SDS-PAGE2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID504135Cytotoxicity against human JMAR cells after 72 hrs by MTS assay2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID502914Cytotoxicity against human PC3M cells assessed as viable cell after 24 hrs by MTT assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID502917Displacement of biotinyl-withaferin from annexin-2 in human CHP100 at 0.4 to 4 uM by chemiluminescence assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID670622Induction of caspase 3 activation in human HeLa cells using Ac-DEVD-pNA at 8 uM after 4 hrs by Bradford assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID774166Activation of Chk1 in human PC3 cells assessed as phosphorylation of CDC25C at Ser2162013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID502902Displacement of biotinyl-withaferin from bovine lung annexin 5 at 10 uM by chemiluminescence assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID1130015Cytotoxicity against human CHP100 cells assessed as inhibition of cell survival at 4 uM after 24 hrs by MTT assay relative to control2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Structure-activity relationships for withanolides as inducers of the cellular heat-shock response.
AID504158Induction of apoptosis in human MDA1986 cells assessed as decrease in procaspase-3 level at 1 to 6 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID1240130Inhibition of BCL-2 expression in human PANC1 cells at 1 uM after 12 hrs by Western blotting2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Hedgehog inhibitors from Withania somnifera.
AID1241663Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation/survival after 72 hrs by resazurin dye reduction assay2015Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
Discovery of Potent 17β-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.
AID360409Reversal of inhibition of TNF-induced NFkappaB/DNA binding in mouse L929sA cells at 2.8 ug/ml in presence of 250 uM dithiothreitol by electrophoretic mobility shift assay2007The Journal of biological chemistry, Feb-16, Volume: 282, Issue:7
Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity.
AID639261Cytotoxicity against human MCR5 cells after 72 hrs by MTS assay2011Journal of natural products, Dec-27, Volume: 74, Issue:12
Cytotoxic withanolide constituents of Physalis longifolia.
AID504154Induction of apoptosis in human JMAR cells assessed as decrease in procaspase-3 level at 1 to 6 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID670619Induction of apoptosis in human HeLa cells assessed as increase in sub-G1 DNA content at 24 uM after 12 hrs using Propidium iodide staining by flow cytometry2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID504138Induction of cell cycle arrest in human MDA1986 cells assessed as accumulation at G2/M phase at 3 uM after 24 hrs by flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504162Inhibition of Akt phosphorylation in human MDA1986 cells after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID502907Effect on human annexin 2-mediated F-actin bundling assessed as increase in light scattering after 1 hr by SDS-PAGE2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID504145Induction of apoptosis in human JHU011 cells assessed as increase in non-viable necrotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504146Induction of apoptosis in human JMAR cells assessed as increase in early apoptotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID639257Cytotoxicity against mouse B16F10 cells after 72 hrs by MTS assay2011Journal of natural products, Dec-27, Volume: 74, Issue:12
Cytotoxic withanolide constituents of Physalis longifolia.
AID1240128Inhibition of BCL-2 expression in human HaCaT cells expressing GLI1 at 1.5 uM after 12 hrs by Western blotting2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Hedgehog inhibitors from Withania somnifera.
AID774174Downregulation of cyclin A2 protein expression in human PC3 cells at IC50 after 12 to 48 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID286449Cytotoxicity against human MCF7 cells by MTT method2007Journal of natural products, May, Volume: 70, Issue:5
Cytotoxic withanolides from Tubocapsicum anomalum.
AID504161Inhibition of Akt phosphorylation in human UM-SCC2 cells after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504163Inhibition of Akt phosphorylation in human JMAR cells after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID1056313Cytotoxicity against human MRC5 cells after 72 hrs by MTS assay2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Synthesis and Cytotoxicity of Semisynthetic Withalongolide A Analogues.
AID774163Upregulation of Aurora B protein expression in human PC3 cells at IC50 after 12 to 48 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID774179Growth inhibition of human DU145 cells assessed as loss of cell viability after 24 hrs by trypan blue exclusion assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID735389Cytotoxicity against human MDA1986 cells after 72 hrs by MTS assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Antiproliferative withanolides from Datura wrightii.
AID774184Upregulation of p21 mRNA expression in human PC3 cells at IC50 after 12 to 48 hrs by SYBR green staining-based RT-PCR analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID504137Induction of cell cycle arrest in human JMAR cells assessed as accumulation at G2/M phase at 3 uM after 24 hrs by flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID502898Displacement of biotinyl-withaferin from bovine lung annexin-2 at 4 uM by chemiluminescence assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID670608Cytotoxicity against african green monkey Vero cells assessed as cell viability after 48 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID735387Cytotoxicity against human MRC5 cells after 72 hrs by MTS assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Antiproliferative withanolides from Datura wrightii.
AID670634Induction of apoptosis in human HeLa cells assessed as phosphatidylserine externalization after 0.5 to 4 hrs using annexin/PI staining by fluorescence microscopy2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID504178Induction of apoptosis in human MDA1986 cells assessed as increase in late apoptotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID774177Induction of cell cycle arrest in human DU145 cells assessed as accumulation at G2/M phase at 1 uM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 22%)2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID286447Cytotoxicity against human HepG2 cells by MTT method2007Journal of natural products, May, Volume: 70, Issue:5
Cytotoxic withanolides from Tubocapsicum anomalum.
AID774162Induction of Aurora B-mediated histone H3 phosphorylation at Ser10 in human PC3 cells after 12 to 48 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID504160Inhibition of Akt phosphorylation in human JHU011 cells after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID396735Cytotoxicity against human MCF7 cells by MTT assay2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
2,3-Dihydrowithaferin A-3beta-O-sulfate, a new potential prodrug of withaferin A from aeroponically grown Withania somnifera.
AID1241664Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation/survival after 72 hrs by resazurin dye reduction assay2015Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
Discovery of Potent 17β-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.
AID264655Ability to block bFGF-induced vessel growth in the type 1 collagen matrix at 1 uM2006Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10
Development of withaferin A analogs as probes of angiogenesis.
AID670616Induction of apoptosis in human HeLa cells assessed as chromatin condensation at 8 uM after 12 hrs using Hoechst 33342 staining by fluorescence microscopic analysis2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID774164Effect on 14-3-3 protein expression in human PC3 cells at IC50 after 12 to 48 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID1130018Induction of HSP90B' (unknown origin)-mediated heat shock response expressed in human 293T cells coexpressing GFP assessed as heat shock index after overnight incubation by luciferase reporter gene assay relative to control2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Structure-activity relationships for withanolides as inducers of the cellular heat-shock response.
AID1241667Cytotoxicity against HFF assessed as inhibition of cell proliferation/survival after 72 hrs by resazurin dye reduction assay2015Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
Discovery of Potent 17β-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.
AID774165Activation of Cdc2/cyclin B in human PC3 cells2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID670611Induction of apoptosis in human HeLa cells assessed as DNA fragmentation at 16 uM after 48 hrs by agarose gel electrophoresis2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID670606Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID504144Induction of apoptosis in human JHU011 cells assessed as mild increase in late apoptotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID396734Growth inhibition of human NCI60 cells2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
2,3-Dihydrowithaferin A-3beta-O-sulfate, a new potential prodrug of withaferin A from aeroponically grown Withania somnifera.
AID1240123Cytotoxicity against human PANC1 cells after 24 hrs by FMCA2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Hedgehog inhibitors from Withania somnifera.
AID1240127Inhibition of PTCH expression in human HaCaT cells expressing GLI1 at 1.5 uM after 12 hrs by Western blotting2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Hedgehog inhibitors from Withania somnifera.
AID504169Inhibition of ERK1/2 phosphorylation in human JHU011 cells at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID670614Induction of apoptosis in human HeLa cells assessed as DNA fragmentation at 4 to 32 uM after 12 hrs by agarose gel electrophoresis2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID774157Inhibition of tubulin-alpha (unknown origin) polymerization by fluorescence-based assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID670629Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 2 to 4 uM up to 4 hrs using annexin/PI staining by fluorescence microscopy2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID504171Inhibition of ERK1/2 phosphorylation in human MDA1986 cells at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID639258Cytotoxicity against human SK-MEL-28 cells after 72 hrs by MTS assay2011Journal of natural products, Dec-27, Volume: 74, Issue:12
Cytotoxic withanolide constituents of Physalis longifolia.
AID1256767Cytotoxicity against human MCF7 cells by MTT assay2015Journal of natural products, Oct-23, Volume: 78, Issue:10
Withanolides and Sucrose Esters from Physalis neomexicana.
AID1130021Toxicity in sc dosed mouse2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Structure-activity relationships for withanolides as inducers of the cellular heat-shock response.
AID502916Displacement of biotinyl-withaferin from annexin-2 in human MCF10A at 0.4 to 4 uM by chemiluminescence assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID504167Inhibition of Akt in human UM-SCC2 cells assessed as decrease in total protein level at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID670609Cytotoxicity against african green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID502895Induction of annexin-2-mediated cytotoxicity in human MCF10A cells assessed as cell morphology at 4 uM after 2 hrs by scanning electron microscopy2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID774169Reduction in CDC2 phosphorylation at Tyr15 in human PC3 cell cytoplasm at 1 uM after 24 hrs by immunofluorescence assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID504179Induction of apoptosis in human MDA1986 cells assessed as increase in non-viable necrotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID1240122Inhibition of hedgehog/GLI1-mediated transcriptional activity in human HaCaT cells after 12 hrs by luciferase assay2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Hedgehog inhibitors from Withania somnifera.
AID504143Induction of apoptosis in human JHU011 cells assessed as early apoptotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID774167Reduction in CHK2 phosphorylation at Thr68 in human PC3 cells at IC50 after 12 to 48 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID670605Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID504165Inhibition of Akt in human MDA1986 cells assessed as decrease in total protein level at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID774172Upregulation of p21 protein expression in human PC3 cells at IC50 after 12 to 48 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID504142Induction of cell cycle arrest in human MDA1986 cells assessed as accumulation at subG0 phase at 3 uM after 24 hrs by flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID774180Induction of cell cycle arrest in human PC3 cells assessed as accumulation at G2/M phase at 1 uM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 28.3%)2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID360412Reduction of IL6 protein level in ip dosed zymosan-induced C57BL/6J mouse inflamed paw model measured 6 hrs after zymosan challenge2007The Journal of biological chemistry, Feb-16, Volume: 282, Issue:7
Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity.
AID735386Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for human U87 cells2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Antiproliferative withanolides from Datura wrightii.
AID774176Induction of cell cycle arrest in human DU145 cells assessed as accumulation at G2/M phase at 1 uM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 22%)2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID504156Induction of apoptosis in human UM-SCC2 cells assessed as decrease in procaspase-3 level at 1 to 6 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504170Inhibition of ERK1/2 phosphorylation in human JMAR cells at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID502904Displacement of biotinyl-withaferin from bovine lung annexin 6 at 10 uM by chemiluminescence assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID502908Induction of annexin 2-mediated F-actin disruption in human WI38 cells at 4 uM after 2 hrs by confocal laser scanning microscopy2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID1056315Cytotoxicity against human JMAR cells after 72 hrs by MTS assay2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Synthesis and Cytotoxicity of Semisynthetic Withalongolide A Analogues.
AID504157Induction of apoptosis in human UM-SCC2 cells assessed as induction of PRAP cleavage after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID735390Cytotoxicity against human U87 cells after 72 hrs by MTS assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Antiproliferative withanolides from Datura wrightii.
AID360411Antiinflammatory activity against ip dosed zymosan-induced C57BL/6J mouse inflamed paw model assessed as effect on paw swelling administered 30 mins before zymosan challenge2007The Journal of biological chemistry, Feb-16, Volume: 282, Issue:7
Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity.
AID502897Displacement of biotinyl-withaferin from bovine lung annexin-2 at 0.4 uM by chemiluminescence assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID670623Increase in caspase 3 activation in human HeLa cells using Ac-DEVD-pNA at 12 uM after 4 hrs by Bradford assay relative to control2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID670627Induction of apoptosis in human HeLa cells assessed as phosphatidylserine externalization at 2 to 16 uM using annexin/PI staining by fluorescence microscopy2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID774155Cell cycle arrest in human DU145 cells assessed as accumulation at G2/M phase at 1 uM after 8 hrs by propidium iodide staining-based flow cytometry2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID670621Induction of caspase 3 activation in human HeLa cells using Ac-DEVD-pNA at 4 uM after 4 hrs by Bradford assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID1241666Cytotoxicity against human SF268 cells assessed as inhibition of cell proliferation/survival after 72 hrs by resazurin dye reduction assay2015Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
Discovery of Potent 17β-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.
AID504168Inhibition of Akt in human JHU011 cells assessed as decrease in total protein level at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504133Cytotoxicity against human UM-SCC2 cells after 72 hrs by MTS assay2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID774160Mitotic arrest in human PC3 cells assessed as accumulation of phosphorylated histone H3 in nucleus by DAPI staining-based confocal microscopic analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID774156Cell cycle arrest in human PC3 cells assessed as accumulation at G2/M phase at 1 uM after 8 hrs by propidium iodide staining-based flow cytometry2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID504148Induction of apoptosis in human JMAR cells assessed as increase in non-viable necrotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID360407Induction of IKK-beta-hyperphosphorylation in IFN-stimulated mouse L929sA cells at 2.8 ug/ml by Western blot2007The Journal of biological chemistry, Feb-16, Volume: 282, Issue:7
Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID396736Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
2,3-Dihydrowithaferin A-3beta-O-sulfate, a new potential prodrug of withaferin A from aeroponically grown Withania somnifera.
AID735388Cytotoxicity against human U251 cells after 72 hrs by MTS assay2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Antiproliferative withanolides from Datura wrightii.
AID286451Cytotoxicity against human MDA-MB-231 cells by MTT method2007Journal of natural products, May, Volume: 70, Issue:5
Cytotoxic withanolides from Tubocapsicum anomalum.
AID774183Reduction in CDC2 phosphorylation at Tyr15 in human PC3 cells at 1 uM after 12 to 24 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID504140Induction of cell cycle arrest in human JHU011 cells assessed as accumulation at G2/M phase at 3 uM after 24 hrs by flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504175Inhibition of ERK1/2 phosphorylation in human JMAR cells assessed as effect on total protein level at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504147Induction of apoptosis in human JMAR cells assessed as increase in late apoptotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504173Inhibition of ERK1/2 phosphorylation in human JHU011 cells assessed as effect on total protein level at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID670635Induction of apoptosis in human HeLa cells assessed as necrotic cells after 0.5 to 4 hrs using annexin/PI staining by fluorescence microscopy2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID639259Cytotoxicity against human JMAR cells after 72 hrs by MTS assay2011Journal of natural products, Dec-27, Volume: 74, Issue:12
Cytotoxic withanolide constituents of Physalis longifolia.
AID286452Cytotoxicity against human MRC5 cells by MTT method2007Journal of natural products, May, Volume: 70, Issue:5
Cytotoxic withanolides from Tubocapsicum anomalum.
AID1240129Inhibition of PTCH expression in human PANC1 cells at 1 uM after 12 hrs by Western blotting2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Hedgehog inhibitors from Withania somnifera.
AID504139Induction of cell cycle arrest in human UM-SCC2 cells assessed as accumulation at G2/M phase at 3 uM after 24 hrs by flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID502899Displacement of biotinyl-withaferin from bovine lung annexin-2 at 40 uM by chemiluminescence assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID1240125Cytotoxicity against human MCF7 cells after 24 hrs by FMCA2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Hedgehog inhibitors from Withania somnifera.
AID1056316Cytotoxicity against human DRO 81-1 cells after 72 hrs by MTS assay2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Synthesis and Cytotoxicity of Semisynthetic Withalongolide A Analogues.
AID670617Induction of apoptosis in human HeLa cells assessed as formation of apoptotic bodies at 8 uM after 12 hrs using Hoechst 33342 staining by fluorescence microscopic analysis2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID504141Induction of cell cycle arrest in human JMAR cells assessed as accumulation at subG0 phase at 3 uM after 24 hrs by flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID774171Reduction in CDC25C phosphorylation at Ser216 in human PC3 cells at 1 uM after 12 to 24 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID360410Reversal of induction of IKK-beta-hyperphosphorylation in IFN-stimulated mouse L929sA cells at 2.8 ug/ml in presence of 5 mM dithiothreitol2007The Journal of biological chemistry, Feb-16, Volume: 282, Issue:7
Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity.
AID502900Displacement of biotinyl-withaferin from bovine lung annexin 1 at 10 uM by chemiluminescence assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID502920Cytotoxicity against human CHP100 cells assessed as viable cell after 24 hrs by MTT assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID502911Cytotoxicity against human HepG2 cells harboring annexin 2 after 48 hrs by MTT assay2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID502915Cytotoxicity against human HepG2 cells harboring annexin 2 assessed as rapid shape change and rounding up at 4 uM after 2 hrs2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID1130019Cytotoxicity against human NCI-H929 cells after 3 days by Alamar blue assay2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Structure-activity relationships for withanolides as inducers of the cellular heat-shock response.
AID670604Cytotoxicity against human HeLa cells assessed as cell viability after 72 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID504151Induction of apoptosis in human UM-SCC2 cells assessed as increase in late non-viable necrotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504150Induction of apoptosis in human UM-SCC2 cells assessed as increase in late apoptotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID670603Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID504176Inhibition of ERK1/2 phosphorylation in human MDA1986 cells assessed as effect on total protein level at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID1240126Cytotoxicity against mouse C3H10T1/2 cells after 24 hrs by FMCA2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Hedgehog inhibitors from Withania somnifera.
AID502905Binding affinity to annexin 2 assessed as inhibition of protein-lipid interaction after 15 mins by coomassine blue staining2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID504155Induction of apoptosis in human JMAR cells assessed as induction of PRAP cleavage after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504172Inhibition of ERK1/2 phosphorylation in human UM-SCC2 cells at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID396739Induction of HSF1-mediated heat-shock protein 72 expression in mouse fibroblast with plasmid EGFP at 2 uM after overnight incubation by micro plate fluorometer2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
2,3-Dihydrowithaferin A-3beta-O-sulfate, a new potential prodrug of withaferin A from aeroponically grown Withania somnifera.
AID504149Induction of apoptosis in human UM-SCC2 cells assessed as increase in early apoptotic cells at 5 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based flow cytometry2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504134Cytotoxicity against human MDA1986 cells after 72 hrs by MTS assay2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID774182Induction of Wee1 phosphorylation at Ser642 in human PC3 cells at 1 uM after 12 to 24 hrs by Western blotting analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID774158Mitotic arrest in human PC3 cells assessed as distorted spindles and curving microtubule array by DAPI staining-based confocal microscopic analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID670628Induction of apoptosis in human HeLa cells assessed as necrotic cells at 2 to 16 uM using annexin/PI staining by fluorescence microscopy2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID1130016Cytotoxicity against human CHP100 cells assessed as inhibition of cell survival after 24 hrs by MTT assay2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Structure-activity relationships for withanolides as inducers of the cellular heat-shock response.
AID1241662Cytotoxicity against human LNCAP cells assessed as inhibition of cell proliferation/survival after 72 hrs by resazurin dye reduction assay2015Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
Discovery of Potent 17β-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.
AID286450Cytotoxicity against human A549 cells by MTT method2007Journal of natural products, May, Volume: 70, Issue:5
Cytotoxic withanolides from Tubocapsicum anomalum.
AID504153Induction of apoptosis in human JHU011 cells assessed as induction of PRAP cleavage after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID504174Inhibition of ERK1/2 phosphorylation in human UM-SCC2 cells assessed as effect on total protein level at 0.1 to 5 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID774159Mitotic arrest in human PC3 cells assessed as defect in depolymerization of tubulin-alpha by DAPI staining-based confocal microscopic analysis2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells.
AID504159Induction of apoptosis in human MDA1986 cells assessed as induction of PRAP cleavage at 1 to 6 uM after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID670620Induction of caspase 3 activation in human HeLa cells using Ac-DEVD-pNA after 4 hrs by Bradford assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID1056314Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTS assay2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Synthesis and Cytotoxicity of Semisynthetic Withalongolide A Analogues.
AID670602Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID670607Cytotoxicity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Withaferin A-related steroids from Withania aristata exhibit potent antiproliferative activity by inducing apoptosis in human tumor cells.
AID396737Induction of F-actin aggregation in human WI38 cells after 4 hrs2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
2,3-Dihydrowithaferin A-3beta-O-sulfate, a new potential prodrug of withaferin A from aeroponically grown Withania somnifera.
AID504164Inhibition of Akt in human MDA1986 cells assessed as highest required for enzyme activity after 24 hrs by Western blot analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Withaferin A, a cytotoxic steroid from Vassobia breviflora, induces apoptosis in human head and neck squamous cell carcinoma.
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID502910Induction of annexin 2-mediated cytoskeleton aggregate accumulation in human HepG2 cells at 4 uM after 2 hrs by confocal laser scanning microscopy2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
AID502912Cytotoxicity against human WI38 cells assessed as cell viability pretreated after 16 hrs by MTT assay in presence of 0.5 uM cytochalasin B2006Nature chemical biology, Jan, Volume: 2, Issue:1
Actin microfilament aggregation induced by withaferin A is mediated by annexin II.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (113)

TimeframeStudies, This Drug (%)All Drugs %
pre-199036 (31.86)18.7374
1990's10 (8.85)18.2507
2000's18 (15.93)29.6817
2010's35 (30.97)24.3611
2020's14 (12.39)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 37.57

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index37.57 (24.57)
Research Supply Index4.91 (2.92)
Research Growth Index4.75 (4.65)
Search Engine Demand Index53.29 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (37.57)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials29 (27.36%)5.53%
Trials0 (0.00%)5.53%
Reviews5 (4.72%)6.00%
Reviews0 (0.00%)6.00%
Case Studies5 (4.72%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other67 (63.21%)84.16%
Other16 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (7)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
DAHANCA 30: A Randomized Non-inferiority Trial of Hypoxia-profile Guided Hypoxic Modification With Nimorazole During Radiotherapy/Chemoradiotherapy of Squamous Cell Carcinoma of the Head and Neck. [NCT02661152]Phase 31,252 participants (Anticipated)Interventional2016-09-30Recruiting
DAHANCA 37 A Phase II Study of Intensity Modulated Proton Therapy (IMPT) for Re-irradiation With Curative Intent for Recurrent or New Primary Head and Neck Cancer [NCT03981068]20 participants (Anticipated)Interventional2019-09-01Recruiting
A Randomised Placebo-controlled Trial of Synchronous NIMorazole Versus RADiotherapy Alone in Patients With Locally Advanced Head and Neck Squamous Cell Carcinoma Not Suitable for Synchronous Chemotherapy or Cetuximab) [NCT01950689]Phase 3338 participants (Actual)Interventional2014-09-11Completed
A Blind Randomized Multicenter Study of Accelerated Fractionated Chemo-radiotherapy With or Without the Hypoxic Cell Radiosensitizer Nimorazole (Nimoral), Using a 15-gene Signature for Hypoxia in the Treatment of Squamous Cell Carcinoma of the Head and Ne [NCT01880359]Phase 3640 participants (Anticipated)Interventional2014-07-25Active, not recruiting
IAEA-HypoX. A Randomized Multicenter Study of Accelerated Fractionated Radiotherapy With or Without the Hypoxic Radiosensitizer Nimorazole in the Treatment of Squamous Cell Carcinoma of the Head and Neck [NCT01507467]Phase 3104 participants (Actual)Interventional2012-03-31Terminated(stopped due to Insufficient recruitment)
Phase I/II Study on Accelerated, Hyperfractionated Radiotherapy With Concomitant Cisplatin and Nimorazole for Patients With Stage III-IV p16 Negative Squamous Cell Cancer (SCC) of the Larynx, Pharynx and Oral Cavity [NCT01733823]Phase 1/Phase 231 participants (Actual)Interventional2013-01-31Completed
Quality of Life After Primary Transoral Robotic Surgery vs Intensity-modulated Radiotherapy for Patients With Early-stage Oropharyngeal Squamous Cell Carcinoma: A Randomized National Trial [NCT04124198]138 participants (Anticipated)Interventional2019-03-01Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]