Page last updated: 2024-12-06

helenalin

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

Description

Helenalin is a sesquiterpene lactone with a unique α-methylene-γ-lactone moiety. It is a potent anti-inflammatory and cytotoxic compound found in various plants of the Asteraceae family, particularly in Arnica montana. Helenalin's synthesis is a complex process that involves multiple enzymatic steps, including the formation of the α-methylene-γ-lactone ring. It is known to inhibit the NF-κB signaling pathway, a key regulator of inflammation, and also possesses anticancer activity by inducing apoptosis. Its cytotoxic effects are attributed to its ability to bind and inactivate various proteins, including kinases and DNA topoisomerases. Helenalin's potent biological activities have made it a subject of extensive research, particularly in the development of new anti-inflammatory and anticancer drugs. The compound's cytotoxicity, however, also poses challenges in its therapeutic application, necessitating strategies to improve its selectivity and reduce its adverse effects.'

helenalin: toxic principle of Helenium microcephalum (smallhead sneezeweed); structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

helenalin : A sesquiterpene lactone that is 3,3a,4,4a,7a,8,9,9a-octahydroazuleno[6,5-b]furan-2,5-dione substituted by a hydroxy group at position 4, methyl groups at positions 4a and 8 and a methylidene group at position 3 (the 3aS,4S,4aR,7aR,8R,9aR stereoisomer). [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]

NF-kappaB inhibitor : An inhibitor of NF-kappaB (nuclear factor kappa-light-chain-enhancer of activated B cells), a protein complex involved in the transcription of DNA. [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]

FloraRankFlora DefinitionFamilyFamily Definition
Microcephalumgenus[no description available]AsteraceaeA large plant family of the order Asterales, subclass Asteridae, class Magnoliopsida. The family is also known as Compositae. Flower petals are joined near the base and stamens alternate with the corolla lobes. The common name of daisy refers to several genera of this family including Aster; CHRYSANTHEMUM; RUDBECKIA; TANACETUM.[MeSH]
Heleniumgenus[no description available]AsteraceaeA large plant family of the order Asterales, subclass Asteridae, class Magnoliopsida. The family is also known as Compositae. Flower petals are joined near the base and stamens alternate with the corolla lobes. The common name of daisy refers to several genera of this family including Aster; CHRYSANTHEMUM; RUDBECKIA; TANACETUM.[MeSH]
Helenium microcephalumspecies[no description available]AsteraceaeA large plant family of the order Asterales, subclass Asteridae, class Magnoliopsida. The family is also known as Compositae. Flower petals are joined near the base and stamens alternate with the corolla lobes. The common name of daisy refers to several genera of this family including Aster; CHRYSANTHEMUM; RUDBECKIA; TANACETUM.[MeSH]
Helenium microcephalumspecies[no description available]AsteraceaeA large plant family of the order Asterales, subclass Asteridae, class Magnoliopsida. The family is also known as Compositae. Flower petals are joined near the base and stamens alternate with the corolla lobes. The common name of daisy refers to several genera of this family including Aster; CHRYSANTHEMUM; RUDBECKIA; TANACETUM.[MeSH]

Cross-References

ID SourceID
PubMed CID23205
CHEMBL ID338474
CHEBI ID5635
SCHEMBL ID161593
MeSH IDM0041461

Synonyms (60)

Synonym
brn 0028081
nsc 85236
hsdb 3490
azuleno(6,5-b)furan-2,5-dione, 3,3a,4,4a,7a,8,9,9a-octahydro-4-hydroxy-4a,8-dimethyl-3-methylene-, (3as-(3aalpha,4alpha,4abeta,7aalpha,8alpha,9aalpha))-
(3as)-3,3aalpha,4alpha,4a,7aalpha,8,9,9aalpha-octahydro-4-hydroxy-4abeta,8 alpha-dimethyl-3-methyleneazuleno(6,5-b)-furan-2,5-dione
ambrosa-2,11(13)-dien-12-oic acid, 6-alpha,8-beta-dihydroxy-4-oxo-, 12,8-lactone
6alpha,8beta-dihydroxy-4-oxoambrosa-2,11(13)-dien-12-oic acid 12,8-lactone
ambrosa-2,11(13)-dien-12-oic acid, 6alpha,8beta-dihydroxy-4-oxo-, 12,8-lactone
NCI60_041870
BSPBIO_001312
azuleno[6,5-dione, 3,3a,4,4a,7a,8,9,9a-octahydro-4-hydroxy-4a,8-dimethyl-3-methylene-, [3as-(3a.alpha.,4.alpha.,4a.beta.,7a.alpha.,8.alpha.,9a.alpha.)]-
wln: t c575 dyvo mv kutj a1 bq du1 i1
nsc-85236
ambrosa-2, 6.alpha.,8.beta.-dihydroxy-4-oxo-, 12,8-lactone
NSC85236 ,
pf 56
azuleno[6,5-b]furan-2,5-dione, 3,3a,4,4a,7a,8,9,9a-octahydro-4-hydroxy-4a,8-dimethyl-3-methylene-, [3as-(3a.alpha.,4.alpha.,4a.beta.,7a.alpha.,8.alpha.,9a.alpha.)]-
ambrosa-2,11(13)-dien-12-oic acid, 6.alpha.,8.beta.-dihydroxy-4-oxo-, 12,8-lactone
4-hydroxy-4a,8-dimethyl-3-methylene-3,3a,4,4a,7a,8,9,9a-octahydroazuleno[6,5-b]furan-2,5-dione
(3ar,5r,5ar,8ar,9s,9as)-9-hydroxy-5,8a-dimethyl-1-methylene-3a,4,5,5a,9,9a-hexahydroazuleno[6,7-b]furan-2,8-dione
helenalin
C09473
6754-13-8
MLS000728512 ,
smr000445626
(3ar,5r,5ar,8ar,9s,9as)-9-hydroxy-5,8a-dimethyl-1-methylidene-3a,4,5,5a,9,9a-hexahydroazuleno[7,6-d]furan-2,8-dione
NCGC00163416-01
NCGC00163416-02
(3ar,5r,5ar,8ar,9s,9as)-9-hydroxy-5,8a-dimethyl-1-methylidene-3a,4,5,5a,9,9a-hexahydroazuleno[6,7-b]furan-2,8-dione
HMS1989B14
CHEMBL338474
chebi:5635 ,
HMS1791B14
HMS2236C04
4-18-00-01434 (beilstein handbook reference)
unii-4guy9l896t
helenalin a
4guy9l896t ,
(3as)-3,3aalpha,4alpha,4a,7aalpha,8,9,9aalpha-octahydro-4-hydroxy-4abeta,8alpha-dimethyl-3-methyleneazuleno(6,5-b)-furan-2,5-dione
(3as,4s,4ar,7ar,8r,9ar)-4-hydroxy-4a,8-dimethyl-3-methylidene-3,3a,4,4a,7a,8,9,9a-octahydroazuleno[6,5-b]furan-2,5-dione
BRD-K26302255-001-02-3
(-)-helenalin
6.alpha.,8.beta.-dihydroxy-4-oxoambrosa-2,11(13)-dien-12-oic acid 12,8-lactone
helenalin [mi]
(3as-(3a.alpha.,4.alpha.,4a.beta.,7a.alpha.,8.alpha.,9a.alpha.))-3,3a,4,4a,7a,8,9,9a-octahydro-4-hydroxy-4a,8-dimethyl-3-methyleneazuleno(6,5-b)furan-2,5-dione
helenalin [hsdb]
SCHEMBL161593
bdbm43484
cid_23205
(3ar,5r,5ar,8ar,9s,9as)-9-hydroxy-5,8a-dimethyl-1-methylene-3a,4,5,5a,9,9a-hexahydroazuleno[6,7-b]furan-2,8-quinone
(3ar,5r,5ar,8ar,9s,9as)-5,8a-dimethyl-1-methylidene-9-oxidanyl-3a,4,5,5a,9,9a-hexahydroazuleno[6,7-b]furan-2,8-dione
HB3927
DTXSID50217868
Q387505
CS-0078850
HY-119970
(3as,4s,4ar,7ar,8r,9ar)-4-hydroxy-4a,8-dimethyl-3-methylene-3,3a,4,4a,7a,8,9,9a-octahydroazuleno[6,5-b]furan-2,5-dione
MS-23694
nf-kappab inhibitor
AKOS040741831

Research Excerpts

Overview

Helenalin is a naturally occuring sesquiterpene lactone extracted from Arnica montana and Arnica chamissonis ssp. Helenalin targets Cys38 within the DNA binding domain of NF-κB transcription factor p65 (RelA)

ExcerptReferenceRelevance
"Helenalin is a pseudoguaianolide natural product that targets Cys38 within the DNA binding domain of NF-κB transcription factor p65 (RelA). "( Helenalin Analogues Targeting NF-κB p65: Thiol Reactivity and Cellular Potency Studies of Varied Electrophiles.
Baur, JW; Brown, DA; Brown, TJ; Edwards, JT; Harki, DA; Kempema, AM; Meece, FA; Skopec, HM; Widen, JC, 2018
)
3.37
"Helenalin is a naturally occuring sesquiterpene lactone extracted from Arnica montana and Arnica chamissonis ssp. "( Helenalin suppresses essential immune functions of activated CD4+ T cells by multiple mechanisms.
Berges, C; Daniel, V; Fuchs, D; Naujokat, C; Opelz, G, 2009
)
3.24
"Helenalin is a potent anti-inflammatory and anti-neoplastic agent isolated from several plant species of the Asteracea family. "( Sesquiterpene lactone helenalin suppresses Leydig and adrenocortical cell steroidogenesis by inhibiting expression of the steroidogenic acute regulatory protein.
Söder, O; Supornsilchai, V; Svechnikov, K, 2006
)
2.09
"Helenalin is a sesquiterpene lactone with potent anti-inflammatory properties."( Helenalin reduces Staphylococcus aureus infection in vitro and in vivo.
Boulanger, D; Brouillette, E; Bureau, F; Jaspar, F; Lekeux, P; Mainil, J; Malouin, F, 2007
)
2.5

Effects

ExcerptReferenceRelevance
"Helenalin has shown its anti-cancer potential to treat multiple types of tumors, both in vitro and in vivo. "( Recent Patents on Anti-Cancer Potential of Helenalin.
Guarve, K; Kriplani, P, 2020
)
2.26

Actions

ExcerptReferenceRelevance
"Helenalin did not inhibit protein kinase C (PKC) and PKC appeared to play a minor role in the effects of helenalin on [Ca2+]i responses in intact cells."( Increased intracellular Ca2+ signaling caused by the antitumor agent helenalin and its analogues.
Abraham, RT; Ashendel, CL; Bonjouklian, R; Gallegos, A; Grindey, GB; Powis, G; Zalkow, LH, 1994
)
1.24

Treatment

ExcerptReferenceRelevance
"Helenalin treatment markedly triggered ROS production and lowered TrxR1 expression, which was ameliorated by ROS inhibitor."( Helenalin Facilitates Reactive Oxygen Species-Mediated Apoptosis and Cell Cycle Arrest by Targeting Thioredoxin Reductase-1 in Human Prostate Cancer Cells.
Li, Y; Wang, F; Yang, M; Yang, Y; Yu, X; Zhang, W; Zhang, Y, 2021
)
2.79

Toxicity

The 14-day LD50 for a single dose of helenalin in male mice was 43 mg/kg. The acetate (2) and isobutyrate (3) were more toxic than helenaline itself. BHM is a pharmacologically active sesquiterpene lactone.

ExcerptReferenceRelevance
"Bis(helenalinyl)malonate [BHM], a pharmacologically active sesquiterpene lactone potentially useful as an antineoplastic agent, proved to be less toxic than its parent compound, helenalin."( Renal, hepatic, cardiac and thymic acute toxicity afforded by bis(helenalinyl)malonate in BDF1 mice.
Chaney, SG; Chang, JJ; Grippo, AA; Hall, IH; Holbrook, DJ; Lee, KH; Yang, LM, 1990
)
1.07
"Helanalin, a sesquiterpene lactone antineoplastic agent, is toxic at therapeutic doses in murine tumors."( Role of thiol agents in protecting against the toxicity of helenalin in tumor-bearing mice.
Grippo, AA; Hall, IH; Holbrook, DJ; Kim, HL; Lee, KH; Lin, HC; Roberts, G, 1989
)
0.52
"Hymenoxon and helenalin are toxic sesquiterpene lactones present in the toxic range plants Hymenoxys odorata and Helenium microcephalum."( Role of glutathione in the toxicity of the sesquiterpene lactones hymenoxon and helenalin.
Hayes, MA; Kim, HL; Merrill, JC; Murray, CA; Safe, S, 1988
)
0.86
" The 14-day LD50 for a single ip dose of helenalin in male mice was 43 mg/kg."( Acute toxicity of helenalin in BDF1 mice.
Chaney, SG; Chang, J; Chapman, DE; Grippo, AA; Hall, IH; Holbrook, DJ; Lee, KH; Reynolds, DJ; Roberts, GB, 1988
)
0.87
" Within a series of helenalin esters, the acetate (2) and isobutyrate (3) were more toxic than helenalin itself (1)."( Structure-cytotoxicity relationships of some helenanolide-type sesquiterpene lactones.
Beekman, AC; Konings, AW; Pras, N; Schmidt, TJ; van Uden, W; Wikström, HV; Woerdenbag, HJ, 1997
)
0.62

Dosage Studied

ExcerptRelevanceReference
" Dose-response experiments in primary cells confirmed pathway selectivity, but importantly also revealed differential inhibition of cell types and new druggability trends across multiple compounds."( High-content single-cell drug screening with phosphospecific flow cytometry.
Clutter, MR; Crane, JM; Krutzik, PO; Nolan, GP, 2008
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
anti-inflammatory agentAny compound that has anti-inflammatory effects.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
plant metaboliteAny eukaryotic metabolite produced during a metabolic reaction in plants, the kingdom that include flowering plants, conifers and other gymnosperms.
metaboliteAny intermediate or product resulting from metabolism. The term 'metabolite' subsumes the classes commonly known as primary and secondary metabolites.
[role 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]

Drug Classes (5)

ClassDescription
gamma-lactoneA lactone having a five-membered lactone ring.
cyclic ketone
organic heterotricyclic compoundAn organic tricyclic compound in which at least one of the rings of the tricyclic skeleton contains one or more heteroatoms.
sesquiterpene lactoneAny member of a diverse class of complex, multicyclic phytochemicals showing a variety of skeleton arrangements and bioactivities, and having in common a sesquiterpenoid structure including a lactone ring.
secondary alcoholA secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it.
[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 (49)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency11.22020.004023.8416100.0000AID485290
glp-1 receptor, partialHomo sapiens (human)Potency2.51190.01846.806014.1254AID624417
thioredoxin reductaseRattus norvegicus (Norway rat)Potency56.23410.100020.879379.4328AID588453
phosphopantetheinyl transferaseBacillus subtilisPotency84.27890.141337.9142100.0000AID1490
ATAD5 protein, partialHomo sapiens (human)Potency9.23990.004110.890331.5287AID504467; AID624247; AID624248; AID624249; AID624250; AID624251; AID624252; AID624253; AID686933; AID686934
USP1 protein, partialHomo sapiens (human)Potency8.91250.031637.5844354.8130AID743255
TDP1 proteinHomo sapiens (human)Potency18.15060.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency14.98230.180013.557439.8107AID1460; AID1468
thioredoxin glutathione reductaseSchistosoma mansoniPotency25.11890.100022.9075100.0000AID485364
Smad3Homo sapiens (human)Potency3.98110.00527.809829.0929AID588855
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency25.11890.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency35.65550.531815.435837.6858AID504845
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency4.46680.28189.721235.4813AID2326
67.9K proteinVaccinia virusPotency10.00000.00018.4406100.0000AID720579; AID720580
glucocerebrosidaseHomo sapiens (human)Potency1.58490.01268.156944.6684AID2101
alpha-galactosidaseHomo sapiens (human)Potency39.81074.466818.391635.4813AID2107
IDH1Homo sapiens (human)Potency1.45810.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.22020.035520.977089.1251AID504332
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency0.79430.01262.451825.0177AID485313
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency35.71680.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency79.43280.006026.168889.1251AID540317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency3.66260.00419.984825.9290AID504444
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency7.94333.548119.542744.6684AID743266
huntingtin isoform 2Homo sapiens (human)Potency2.23870.000618.41981,122.0200AID1688
DNA polymerase betaHomo sapiens (human)Potency100.00000.022421.010289.1251AID485314
mitogen-activated protein kinase 1Homo sapiens (human)Potency31.62280.039816.784239.8107AID1454
ras-related protein Rab-9AHomo sapiens (human)Potency1.00000.00022.621531.4954AID485297
DNA polymerase eta isoform 1Homo sapiens (human)Potency89.12510.100028.9256213.3130AID588591
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency14.12540.050127.073689.1251AID588590
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency3.16230.00798.23321,122.0200AID2546; AID2551
gemininHomo sapiens (human)Potency0.53290.004611.374133.4983AID624296; AID624297
survival motor neuron protein isoform dHomo sapiens (human)Potency0.00560.125912.234435.4813AID1458
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency25.11890.251215.843239.8107AID504327
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency0.56230.058010.694926.6086AID602310
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
photoreceptor-specific nuclear receptorHomo sapiens (human)IC50 (µMol)1.92100.03742.93408.9620AID624394
XBP1Homo sapiens (human)IC50 (µMol)2.43000.16005.404910.0000AID504313
type-1 angiotensin II receptorHomo sapiens (human)IC50 (µMol)18.63902.22108.230418.7980AID463214
apelin receptorHomo sapiens (human)IC50 (µMol)21.30001.75003.39008.3500AID2784
G-protein coupled receptor 55Homo sapiens (human)IC50 (µMol)2.64230.12502.58609.7907AID2013
DNA damage-inducible transcript 3 proteinMus musculus (house mouse)IC50 (µMol)2.61000.16003.995910.0000AID504322
transactivating tegument protein VP16 [Human herpesvirus 1]Human alphaherpesvirus 1 (Herpes simplex virus type 1)IC50 (µMol)4.37400.94604.70169.4870AID624395
Transcriptional activator MybGallus gallus (chicken)IC50 (µMol)2.37070.62522.76989.5499AID746038
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
E3 ubiquitin-protein ligase Mdm2 isoform aHomo sapiens (human)EC50 (µMol)0.57000.0800478.57894,301.1099AID1394; AID1442; AID1444
Substance-K receptorRattus norvegicus (Norway rat)EC50 (µMol)0.18000.00050.49643.1300AID1444
[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)
cystic fibrosis transmembrane conductance regulator ATP-binding cassette sub-family C member 7Homo sapiens (human)AC500.98900.039815.002550.0000AID743267
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)IC100 (µMol)10.000010.000010.000010.0000AID242927
Nuclear factor NF-kappa-B p100 subunit Homo sapiens (human)IC100 (µMol)10.000010.000010.000010.0000AID242927
Transcription factor p65Homo sapiens (human)IC100 (µMol)10.00005.00009.000010.0000AID242927; AID262798
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (109)

Processvia Protein(s)Taxonomy
regulation of gene expressionTranscriptional activator MybGallus gallus (chicken)
mitotic cell cycleTranscriptional activator MybGallus gallus (chicken)
positive regulation of transcription by RNA polymerase IITranscriptional activator MybGallus gallus (chicken)
negative regulation of transcription by RNA polymerase IINuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cellular response to lipopolysaccharideNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
transcription by RNA polymerase IINuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
apoptotic processNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
inflammatory responseNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
canonical NF-kappaB signal transductionNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
JNK cascadeNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
negative regulation of gene expressionNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
positive regulation of lipid storageNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
negative regulation of calcidiol 1-monooxygenase activityNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
negative regulation of vitamin D biosynthetic processNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
negative regulation of cholesterol transportNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
negative regulation of interleukin-12 productionNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
response to muscle stretchNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
non-canonical NF-kappaB signal transductionNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
negative regulation of apoptotic processNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
negative regulation of inflammatory responseNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
B cell receptor signaling pathwayNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
negative regulation of protein metabolic processNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
mammary gland involutionNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
positive regulation of transcription initiation by RNA polymerase IINuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cellular response to mechanical stimulusNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cellular response to nicotineNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cellular response to interleukin-1Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cellular response to interleukin-6Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cellular response to tumor necrosis factorNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cellular response to dsRNANuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cellular response to interleukin-17Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cellular response to virusNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
antibacterial innate immune responseNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
positive regulation of hyaluronan biosynthetic processNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cellular response to angiotensinNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
positive regulation of miRNA metabolic processNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cellular response to stressNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
innate immune responseNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
response to cytokineNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
follicular dendritic cell differentiationNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
germinal center formationNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
regulation of DNA-templated transcriptionNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
canonical NF-kappaB signal transductionNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
extracellular matrix organizationNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
response to lipopolysaccharideNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
rhythmic processNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
spleen developmentNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
cellular response to stressNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
innate immune responseNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
non-canonical NF-kappaB signal transductionNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
response to cytokineNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
inflammatory responseNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
positive regulation of interleukin-1 beta productionTranscription factor p65Homo sapiens (human)
positive regulation of interleukin-6 productionTranscription factor p65Homo sapiens (human)
positive regulation of interleukin-8 productionTranscription factor p65Homo sapiens (human)
positive regulation of amyloid-beta formationTranscription factor p65Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activityTranscription factor p65Homo sapiens (human)
nucleotide-binding oligomerization domain containing 2 signaling pathwayTranscription factor p65Homo sapiens (human)
negative regulation of transcription by RNA polymerase IITranscription factor p65Homo sapiens (human)
liver developmentTranscription factor p65Homo sapiens (human)
hair follicle developmentTranscription factor p65Homo sapiens (human)
defense response to tumor cellTranscription factor p65Homo sapiens (human)
response to ischemiaTranscription factor p65Homo sapiens (human)
acetaldehyde metabolic processTranscription factor p65Homo sapiens (human)
chromatin organizationTranscription factor p65Homo sapiens (human)
DNA-templated transcriptionTranscription factor p65Homo sapiens (human)
regulation of DNA-templated transcriptionTranscription factor p65Homo sapiens (human)
regulation of transcription by RNA polymerase IITranscription factor p65Homo sapiens (human)
inflammatory responseTranscription factor p65Homo sapiens (human)
cellular defense responseTranscription factor p65Homo sapiens (human)
neuropeptide signaling pathwayTranscription factor p65Homo sapiens (human)
canonical NF-kappaB signal transductionTranscription factor p65Homo sapiens (human)
positive regulation of cell population proliferationTranscription factor p65Homo sapiens (human)
response to xenobiotic stimulusTranscription factor p65Homo sapiens (human)
animal organ morphogenesisTranscription factor p65Homo sapiens (human)
response to UV-BTranscription factor p65Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionTranscription factor p65Homo sapiens (human)
positive regulation of gene expressionTranscription factor p65Homo sapiens (human)
positive regulation of Schwann cell differentiationTranscription factor p65Homo sapiens (human)
negative regulation of angiogenesisTranscription factor p65Homo sapiens (human)
cytokine-mediated signaling pathwayTranscription factor p65Homo sapiens (human)
protein catabolic processTranscription factor p65Homo sapiens (human)
response to muramyl dipeptideTranscription factor p65Homo sapiens (human)
response to progesteroneTranscription factor p65Homo sapiens (human)
positive regulation of interleukin-12 productionTranscription factor p65Homo sapiens (human)
positive regulation of interleukin-6 productionTranscription factor p65Homo sapiens (human)
positive regulation of interleukin-8 productionTranscription factor p65Homo sapiens (human)
response to insulinTranscription factor p65Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayTranscription factor p65Homo sapiens (human)
negative regulation of protein sumoylationTranscription factor p65Homo sapiens (human)
response to cobalaminTranscription factor p65Homo sapiens (human)
toll-like receptor 4 signaling pathwayTranscription factor p65Homo sapiens (human)
intracellular signal transductionTranscription factor p65Homo sapiens (human)
cellular response to hepatocyte growth factor stimulusTranscription factor p65Homo sapiens (human)
response to muscle stretchTranscription factor p65Homo sapiens (human)
non-canonical NF-kappaB signal transductionTranscription factor p65Homo sapiens (human)
vascular endothelial growth factor signaling pathwayTranscription factor p65Homo sapiens (human)
prolactin signaling pathwayTranscription factor p65Homo sapiens (human)
negative regulation of protein catabolic processTranscription factor p65Homo sapiens (human)
negative regulation of apoptotic processTranscription factor p65Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionTranscription factor p65Homo sapiens (human)
response to amino acidTranscription factor p65Homo sapiens (human)
negative regulation of DNA-templated transcriptionTranscription factor p65Homo sapiens (human)
positive regulation of DNA-templated transcriptionTranscription factor p65Homo sapiens (human)
positive regulation of transcription by RNA polymerase IITranscription factor p65Homo sapiens (human)
negative regulation of insulin receptor signaling pathwayTranscription factor p65Homo sapiens (human)
regulation of inflammatory responseTranscription factor p65Homo sapiens (human)
positive regulation of T cell receptor signaling pathwayTranscription factor p65Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activityTranscription factor p65Homo sapiens (human)
response to cAMPTranscription factor p65Homo sapiens (human)
defense response to virusTranscription factor p65Homo sapiens (human)
cellular response to hydrogen peroxideTranscription factor p65Homo sapiens (human)
interleukin-1-mediated signaling pathwayTranscription factor p65Homo sapiens (human)
response to interleukin-1Transcription factor p65Homo sapiens (human)
cellular response to lipopolysaccharideTranscription factor p65Homo sapiens (human)
cellular response to lipoteichoic acidTranscription factor p65Homo sapiens (human)
cellular response to peptidoglycanTranscription factor p65Homo sapiens (human)
cellular response to nicotineTranscription factor p65Homo sapiens (human)
cellular response to interleukin-1Transcription factor p65Homo sapiens (human)
cellular response to interleukin-6Transcription factor p65Homo sapiens (human)
cellular response to tumor necrosis factorTranscription factor p65Homo sapiens (human)
postsynapse to nucleus signaling pathwayTranscription factor p65Homo sapiens (human)
antiviral innate immune responseTranscription factor p65Homo sapiens (human)
negative regulation of non-canonical NF-kappaB signal transductionTranscription factor p65Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionTranscription factor p65Homo sapiens (human)
negative regulation of miRNA transcriptionTranscription factor p65Homo sapiens (human)
positive regulation of miRNA transcriptionTranscription factor p65Homo sapiens (human)
cellular response to angiotensinTranscription factor p65Homo sapiens (human)
positive regulation of leukocyte adhesion to vascular endothelial cellTranscription factor p65Homo sapiens (human)
positive regulation of miRNA metabolic processTranscription factor p65Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayTranscription factor p65Homo sapiens (human)
cellular response to stressTranscription factor p65Homo sapiens (human)
response to cytokineTranscription factor p65Homo sapiens (human)
innate immune responseTranscription factor p65Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (28)

Processvia Protein(s)Taxonomy
protein bindingTranscriptional activator MybGallus gallus (chicken)
DNA-binding transcription factor activity, RNA polymerase II-specificTranscriptional activator MybGallus gallus (chicken)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTranscriptional activator MybGallus gallus (chicken)
transcription cis-regulatory region bindingNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
chromatin bindingNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
DNA-binding transcription factor activityNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
transcription coregulator activityNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
protein bindingNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
identical protein bindingNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
actinin bindingNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
DNA-binding transcription factor activityNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
protein bindingNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
transcription cis-regulatory region bindingTranscription factor p65Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingTranscription factor p65Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTranscription factor p65Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA bindingTranscription factor p65Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificTranscription factor p65Homo sapiens (human)
transcription coactivator bindingTranscription factor p65Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificTranscription factor p65Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificTranscription factor p65Homo sapiens (human)
DNA bindingTranscription factor p65Homo sapiens (human)
chromatin bindingTranscription factor p65Homo sapiens (human)
DNA-binding transcription factor activityTranscription factor p65Homo sapiens (human)
protein bindingTranscription factor p65Homo sapiens (human)
enzyme bindingTranscription factor p65Homo sapiens (human)
protein kinase bindingTranscription factor p65Homo sapiens (human)
chromatin DNA bindingTranscription factor p65Homo sapiens (human)
ubiquitin protein ligase bindingTranscription factor p65Homo sapiens (human)
peptide bindingTranscription factor p65Homo sapiens (human)
phosphate ion bindingTranscription factor p65Homo sapiens (human)
identical protein bindingTranscription factor p65Homo sapiens (human)
protein homodimerization activityTranscription factor p65Homo sapiens (human)
actinin bindingTranscription factor p65Homo sapiens (human)
histone deacetylase bindingTranscription factor p65Homo sapiens (human)
NF-kappaB bindingTranscription factor p65Homo sapiens (human)
ankyrin repeat bindingTranscription factor p65Homo sapiens (human)
general transcription initiation factor bindingTranscription factor p65Homo sapiens (human)
DNA-binding transcription factor bindingTranscription factor p65Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
nucleoplasmTranscriptional activator MybGallus gallus (chicken)
nucleusTranscriptional activator MybGallus gallus (chicken)
extracellular regionNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
nucleusNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
nucleoplasmNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cytoplasmNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
mitochondrionNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cytosolNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
secretory granule lumenNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
specific granule lumenNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
chromatinNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
transcription regulator complexNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
I-kappaB/NF-kappaB complexNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
nucleusNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
cytoplasmNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
NF-kappaB p50/p65 complexNuclear factor NF-kappa-B p105 subunitHomo sapiens (human)
nucleusNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
nucleoplasmNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
cytoplasmNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
cytosolNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
chromatinNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
Bcl3/NF-kappaB2 complexNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
cytoplasmNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
nucleusNuclear factor NF-kappa-B p100 subunit Homo sapiens (human)
nucleolusTranscription factor p65Homo sapiens (human)
nucleusTranscription factor p65Homo sapiens (human)
glutamatergic synapseTranscription factor p65Homo sapiens (human)
nucleusTranscription factor p65Homo sapiens (human)
nucleoplasmTranscription factor p65Homo sapiens (human)
cytoplasmTranscription factor p65Homo sapiens (human)
cytosolTranscription factor p65Homo sapiens (human)
NF-kappaB p50/p65 complexTranscription factor p65Homo sapiens (human)
NF-kappaB complexTranscription factor p65Homo sapiens (human)
chromatinTranscription factor p65Homo sapiens (human)
transcription regulator complexTranscription factor p65Homo sapiens (human)
cytoplasmTranscription factor p65Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (118)

Assay IDTitleYearJournalArticle
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID110556Antileukemic activity of compound against the P-388 lymphocytic leukemic BDF1 male mice at 8(mg/kg)/day, administered intraperitoneally; 15.7/9.66 (Treated/control)1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Antitumor agents. 44. Bis(helenalinyl) esters and related derivatives as novel potent antileukemic agents.
AID400914Cytotoxicity against human Jurkat T cells2004Journal of natural products, Apr, Volume: 67, Issue:4
New chromanone acids with antibacterial activity from Calophyllum brasiliense.
AID380086Cytotoxicity against human Jurkat T cells after 20 hrs by WST1 assay2006Journal of natural products, Feb, Volume: 69, Issue:2
Cytotoxic diacetylenic spiroketal enol ethers from Plagius flosculosus.
AID380544Cytotoxicity against human ZR-75-1 cells after 48 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID746038Inhibition of c-Myb-induced mim-1 gene expression in doxycyclin-treated chicken HD11 cells after 24 hrs by GFP assay2013European journal of medicinal chemistry, May, Volume: 63Natural sesquiterpene lactones as inhibitors of Myb-dependent gene expression: structure-activity relationships.
AID1149587Antitumor activity against mouse EAC cells allografted in CF1 mouse assessed as [methyl-14C]thymidine incorporation to DNA at 0.125 mg/day administered from day 5 to day 7 measured on day 8 by scintillation counting analysis relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID492467Cytotoxicity against human HepG2 cells2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach.
AID492425Antimalarial activity against Plasmodium falciparum2009Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
Antimalarials from nature.
AID1132951Cytotoxicity against human Hep2 cells assessed a growth inhibition by rapid microtiter technique1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Antitumor agents 32. Synthesis and antitumor activity of cyclopentenone derivatives related to helenalin.
AID1149578Stability of the compound assessed as reactivity with reduced glutathione at 10 mg after 4 hrs by NMR analysis1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID235489Selectivity index is the ratio of MG MID value for all cell lines to that of leukemic cells2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Sequential cytotoxicity: a theory evaluated using novel 2-[4-(3-aryl-2-propenoyloxy)phenylmethylene]cyclohexanones and related compounds.
AID1149567Antitumor activity against mouse EAC cells allografted in CF1 mouse assessed as tumor growth inhibition at 33.3 mg/kg/day, ip after 7 days1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID380523Cytotoxicity against human A431 cells after 48 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID1149595Antitumor activity against mouse EAC cells allografted in CF1 mouse assessed as [gamma-32P] incorporation into nonhistone at 0.125 mg/day administered from day 5 to day 7 measured on day 8 relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID401843Cytotoxicity against mouse cloned EN2 cells after 72 hrs by MTT assay1997Journal of natural products, Mar, Volume: 60, Issue:3
Structure-cytotoxicity relationships of some helenanolide-type sesquiterpene lactones.
AID492468Antitumor activity against mouse P388 cells allografted in mouse at 8 mg/kg relative to control2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach.
AID1149583Antitumor activity against mouse EAC cells allografted in CF1 mouse assessed as DNA content at 0.125 mg/day administered from day 5 to day 7 measured on day 8 by UV-spectrophotometry relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID380520Cytotoxicity against human HL-60 cells after 5 hrs by MTT assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID380518Cytotoxicity against human GTB cells after 5 hrs by MTT assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID380537Cytotoxicity against human SK37 cells after 24 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID1149568Antitumor activity against rat Walker 256 cells allografted in Sprague-Dawley rat at 2.5 mg/kg/day, ip relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID310936Cytotoxicity against human KB cells2007Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8
Quantitative structure-activity relationship of sesquiterpene lactones with cytotoxic activity.
AID1149575Binding affinity to DNA (unknown origin) at 0.015 ug at pH 7.2 after 24 hrs by UV-spectrophotometry1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID262798Inhibition of NF-kappaB DNA binding by EMSA2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Development of a structural model for NF-kappaB inhibition of sesquiterpene lactones using self-organizing neural networks.
AID1149570Cytotoxicity against human Hep2 cells1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID1132873Antitumor activity against mouse P388 cells allografted in DBA/2 mouse assessed as survival rate at 16.8 mg/kg relative to control1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Antitumor agents. 31. Helenalin sym-dimethylethylenediamine reaction products and related derivatives.
AID380528Cytotoxicity against human MCF7 cells after 24 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID99422Mean graph mid point was measured on leukemic cells.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Sequential cytotoxicity: a theory evaluated using novel 2-[4-(3-aryl-2-propenoyloxy)phenylmethylene]cyclohexanones and related compounds.
AID380545Cytotoxicity against human ZR-75-1 cells after 72 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID387024Cytotoxicity against human KB cells2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Use of self-organizing maps and molecular descriptors to predict the cytotoxic activity of sesquiterpene lactones.
AID1149598Antitumor activity against mouse EAC cells allografted in CF1 mouse assessed as ascitocrit count per mililitre of fluid at 0.125 mg/day administered from day 5 to day 7 measured on day 8 by hemocytometry relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID50735Mean graph mid point was measured on colon cancer cells.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Sequential cytotoxicity: a theory evaluated using novel 2-[4-(3-aryl-2-propenoyloxy)phenylmethylene]cyclohexanones and related compounds.
AID1149585Antitumor activity against mouse EAC cells allografted in CF1 mouse assessed as chromatin protein content at 0.125 mg/day administered from day 5 to day 7 measured on day 8 relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID121642In vivo antileukemic activity against P-388 lymphocytic leukemia in BDF1 male mice at 3(mg/kg)/day intraperitoneal dose expressed as T/C1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Antitumor agents. 44. Bis(helenalinyl) esters and related derivatives as novel potent antileukemic agents.
AID380535Cytotoxicity against human SK MEL28 cells after 48 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID110402Antileukemic activity of compound against the P-388 lymphocytic leukemic BDF1 male mice at 25(mg/kg)/day, administered intraperitoneally; 12.3/9.66 (Treated/control)1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Antitumor agents. 44. Bis(helenalinyl) esters and related derivatives as novel potent antileukemic agents.
AID380534Cytotoxicity against human SK MEL28 cells after 24 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID235488Selectivity index is the ratio of MG MID value for all cell lines to that of colon cancer cells2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Sequential cytotoxicity: a theory evaluated using novel 2-[4-(3-aryl-2-propenoyloxy)phenylmethylene]cyclohexanones and related compounds.
AID1149574Binding affinity to dATP (unknown origin) at 0.015 ug by UV-spectrophotometry1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID110559Antileukemic activity of compound against the P-388 lymphocytic leukemic BDF1 male mice at 15(mg/kg)/day, administered intraperitoneally; 11.9/9.66 (Treated/control)1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Antitumor agents. 44. Bis(helenalinyl) esters and related derivatives as novel potent antileukemic agents.
AID380533Cytotoxicity against human OVCAR-3 cells after 72 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID110406Antileukemic activity of compound against the P-388 lymphocytic leukemic BDF1 male mice at 3(mg/kg)/day, administered intraperitoneally; 12.9/9.66 (Treated/control)1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Antitumor agents. 44. Bis(helenalinyl) esters and related derivatives as novel potent antileukemic agents.
AID174706Cytoprotective effect at an oral dose of 40 mg/kg1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
Structure-activity relationship in the gastric cytoprotective effect of several sesquiterpene lactones.
AID495066Inhibition of anisomycin-induced p38 phosphorylation in human U937 cells by Phospho-Flow cytometry at 20 uM2008Nature chemical biology, Feb, Volume: 4, Issue:2
High-content single-cell drug screening with phosphospecific flow cytometry.
AID1132872Cytotoxicity against human Hep2 cells assessed as growth inhibition by microtiter method1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Antitumor agents. 31. Helenalin sym-dimethylethylenediamine reaction products and related derivatives.
AID495065Inhibition of JAK-mediated interferon-gamma-induced Stat1 phosphorylation in human U937 cells by Phospho-Flow cytometry at 20 uM2008Nature chemical biology, Feb, Volume: 4, Issue:2
High-content single-cell drug screening with phosphospecific flow cytometry.
AID1149591Antitumor activity against mouse EAC cells allografted in CF1 mouse assessed as free lysosomal DNAse activity at 0.125 mg/day administered from day 5 to day 7 measured on day 8 relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID1149573Binding affinity to dAMP (unknown origin) at 0.015 ug by UV-spectrophotometry1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID380087Cytotoxicity against human Jurkat T cells overexpressing Bcl2 after 20 hrs by WST1 assay2006Journal of natural products, Feb, Volume: 69, Issue:2
Cytotoxic diacetylenic spiroketal enol ethers from Plagius flosculosus.
AID1149589Antitumor activity against mouse EAC cells allografted in CF1 mouse assessed as nuclear DNA polymerase activity at 0.125 mg/day administered from day 5 to day 7 measured on day 8 relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID380525Cytotoxicity against human HEP2 cells after 24 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID1149576Binding affinity to dGMP (unknown origin) by NMR analysis1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID1149577Stability of the compound assessed as reactivity with oxidized glutathione at 10 mg after 4 hrs by NMR analysis1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID1132871Toxicity in Sprague-Dawley rat allografted with rat Walker 256 cells assessed as mortality after 4 days1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Antitumor agents. 31. Helenalin sym-dimethylethylenediamine reaction products and related derivatives.
AID1149601Antitumor activity against mouse EAC cells assessed as tissue SH stimulation at 0.6 mg measured on day 8 by Ellman method relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID1132952Antitumor activity against mouse P388 cells allografted in DBA/2 mouse assessed as increase in survival rate at 16.8 mg/kg/day, ip administered for 2 weeks relative to control1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Antitumor agents 32. Synthesis and antitumor activity of cyclopentenone derivatives related to helenalin.
AID242927Concentration required for complete inhibition of Nuclear factor kappa B DNA binding2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Quantitative structure-activity relationship of sesquiterpene lactones as inhibitors of the transcription factor NF-kappaB.
AID1149600Antitumor activity against mouse EAC cells assessed as nuclear DNA polymerase activity at 0.6 mg measured on day 8 relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID671223Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by SRB assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Enantiomeric derivatives of tokinolide B: absolute configuration and biological properties.
AID91673Mean graph mid point was measured on all cell lines.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Sequential cytotoxicity: a theory evaluated using novel 2-[4-(3-aryl-2-propenoyloxy)phenylmethylene]cyclohexanones and related compounds.
AID380538Cytotoxicity against human SK37 cells after 48 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID380531Cytotoxicity against human OVCAR-3 cells after 24 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID335952Antiulcerogenic activity in Wistar rat assessed as cytoprotection against ethanol-induced gastric lesions at 40 mg/kg administered 60 mins before ethanol challenge
AID380541Cytotoxicity against human SW872 cells after 48 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID1149596Antitumor activity against mouse EAC cells allografted in CF1 mouse assessed as 3',5' cAMP level at 0.125 mg/day administered from day 5 to day 7 measured on day 8 by RIA relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID121648In vivo antileukemic activity against P-388 lymphocytic leukemia in BDF1 male mice at 8(mg/kg)/day intraperitoneal dose expressed as T/C1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Antitumor agents. 44. Bis(helenalinyl) esters and related derivatives as novel potent antileukemic agents.
AID380539Cytotoxicity against human SK37 cells after 72 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID380529Cytotoxicity against human MCF7 cells after 48 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID671225Cytotoxicity against human SKLU1 cells assessed as growth inhibition after 48 hrs by SRB assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Enantiomeric derivatives of tokinolide B: absolute configuration and biological properties.
AID746037Cytotoxicity against chicken HD11 cells assessed as cell viability after 24 hrs by MTS assay2013European journal of medicinal chemistry, May, Volume: 63Natural sesquiterpene lactones as inhibitors of Myb-dependent gene expression: structure-activity relationships.
AID110545Antileukemic activity of compound against the P-388 lymphocytic leukemic BDF1 male mice at 60 mg/kg/day, administered intraperitoneally; 3.0/9.66 (Treated/control)1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Antitumor agents. 44. Bis(helenalinyl) esters and related derivatives as novel potent antileukemic agents.
AID1464921Cytotoxicity against human HeLa cells by MTT assay2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Cytotoxic properties of the alkaloid rutaecarpine and its oligocyclic derivatives and chemical modifications to enhance water-solubility.
AID380527Cytotoxicity against human HEP2 cells after 72 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID671224Cytotoxicity against human HCT15 cells assessed as growth inhibition after 48 hrs by SRB assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Enantiomeric derivatives of tokinolide B: absolute configuration and biological properties.
AID380522Cytotoxicity against human A431 cells after 24 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID1149569Antitumor activity against mouse P388 cells allografted in DBA/2 mouse at 25 mg/kg/day, ip relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID1132956Antitumor activity against mouse Walker 256 cells allografted in Sprague-Dawley rat assessed as increase in survival rate at 2.5 mg/kg/day, ip relative to control1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Antitumor agents 32. Synthesis and antitumor activity of cyclopentenone derivatives related to helenalin.
AID1149602Antitumor activity against mouse EAC cells allografted in CF1 mouse assessed as cell viability at 0.125 mg/day administered from day 5 to day 7 measured on day 8 by trypan blue assay relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID1149593Antitumor activity against mouse EAC cells allografted in CF1 mouse assessed as [gamma-32P] incorporation into histone at 0.125 mg/day administered from day 5 to day 7 measured on day 8 relative to control1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID380542Cytotoxicity against human SW872 cells after 72 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID492466Antitumor activity against rat Walker 256 cells allografted in rat at 2.5 mg/kg relative to control2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach.
AID121633In vivo antileukemic activity against P-388 Lymphocytic Leukemia in BDF1 male mice at 15(mg/kg)/day intraperitoneal dose expressed as T/C1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Antitumor agents. 44. Bis(helenalinyl) esters and related derivatives as novel potent antileukemic agents.
AID380084Cytotoxicity against human HL60 after 20 hrs by WST1 assay2006Journal of natural products, Feb, Volume: 69, Issue:2
Cytotoxic diacetylenic spiroketal enol ethers from Plagius flosculosus.
AID1149579Stability of the compound assessed as reactivity with L-cysteine at 10 mg after 4 hrs by NMR analysis1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID121635In vivo antileukemic activity against P-388 Lymphocytic Leukemia in BDF1 male mice at 60 mg/kg/day intraperitoneal dose expressed as T/C1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Antitumor agents. 44. Bis(helenalinyl) esters and related derivatives as novel potent antileukemic agents.
AID380540Cytotoxicity against human SW872 cells after 24 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID380530Cytotoxicity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID1132878Toxicity in DBA/2 mouse allografted with mouse P388 cells assessed as mortality after 4 days1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Antitumor agents. 31. Helenalin sym-dimethylethylenediamine reaction products and related derivatives.
AID380536Cytotoxicity against human SK MEL28 cells after 72 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID401842Cytotoxicity against mouse cloned EN2 cells after 2 hrs by MTT assay1997Journal of natural products, Mar, Volume: 60, Issue:3
Structure-cytotoxicity relationships of some helenanolide-type sesquiterpene lactones.
AID380543Cytotoxicity against human ZR-75-1 cells after 24 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID320961Inhibition of serotonin release in bovine platelets2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Neural networks as valuable tools to differentiate between sesquiterpene lactones' inhibitory activity on serotonin release and on NF-kappaB.
AID1132879Antitumor activity against rat Walker 256 cells allografted in Sprague-Dawley rat assessed as survival rate at 2.5 mg/kg relative to control1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Antitumor agents. 31. Helenalin sym-dimethylethylenediamine reaction products and related derivatives.
AID1149571Binding affinity to dGMP (unknown origin) at 0.015 ug at pH 7.2 after 24 hrs by UV-spectrophotometry1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID355111Antineoplastic activity against mouse P388 cells at 3 mg/kg relative to control1996Journal of natural products, Aug, Volume: 59, Issue:8
Progress in the discovery of biosynthetic anticancer drugs.
AID380524Cytotoxicity against human A431 cells after 72 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
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.
AID121634In vivo antileukemic activity against P-388 Lymphocytic Leukemia in BDF1 male mice at 25(mg/kg)/day intraperitoneal dose expressed as T/C1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Antitumor agents. 44. Bis(helenalinyl) esters and related derivatives as novel potent antileukemic agents.
AID495064Inhibition of JAK-mediated GM-CSF-induced Stat5 phosphorylation in human U937 cells by Phospho-Flow cytometry at 20 uM2008Nature chemical biology, Feb, Volume: 4, Issue:2
High-content single-cell drug screening with phosphospecific flow cytometry.
AID1149572Binding affinity to dGTP (unknown origin) at 0.015 ug at pH 7.2 after 24 hrs by UV-spectrophotometry1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antitumor agents. 21. A proposed mechanism for inhibition of cancer growth by tenulin and helenalin and related cyclopentenones.
AID380532Cytotoxicity against human OVCAR-3 cells after 48 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
AID380526Cytotoxicity against human HEP2 cells after 48 hrs by [3H]thymidine incorporation assay1999Journal of natural products, Jul, Volume: 62, Issue:7
Cytotoxic activities of hypocretenolides from Leontodon hispidus.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (146)

TimeframeStudies, This Drug (%)All Drugs %
pre-199031 (21.23)18.7374
1990's16 (10.96)18.2507
2000's49 (33.56)29.6817
2010's40 (27.40)24.3611
2020's10 (6.85)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 38.32

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 Index38.32 (24.57)
Research Supply Index5.02 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index54.12 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (38.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.67%)5.53%
Reviews6 (4.03%)6.00%
Case Studies1 (0.67%)4.05%
Observational0 (0.00%)0.25%
Other141 (94.63%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]