Page last updated: 2024-12-04

carbazilquinone

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Description

Carbazilquinone is a quinone derivative with an intriguing chemical structure and potential biological activity. It is synthesized through a multi-step process that involves the oxidation of carbazole, a heterocyclic compound. Research on carbazilquinone is driven by its potential as an anticancer agent. Studies have indicated that it exhibits cytotoxic effects against various cancer cell lines, possibly due to its ability to induce apoptosis and inhibit tumor growth. Its mode of action is still under investigation, but it is believed to involve the generation of reactive oxygen species (ROS) and the disruption of mitochondrial function. Carbazilquinone's potential therapeutic benefits are further supported by its ability to target cancer cells selectively, sparing normal cells. Despite promising initial findings, further research is necessary to fully understand its pharmacological profile, including its safety and efficacy in preclinical and clinical settings.'

Carbazilquinone: An alkylating agent structurally similar to MITOMYCIN and found to be effective in the treatment of leukemia and various other neoplasms in mice. It causes leukemia and thrombocytopenia in almost all human patients. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2569
CHEMBL ID443014
CHEBI ID31356
SCHEMBL ID8079
MeSH IDM0003336

Synonyms (54)

Synonym
smr001566820
CHEMBL443014
2,4-dione, 2-[2-[(aminocarbonyl)oxy]-1-methoxyethyl]-3,6-bis(1-aziridinyl)-5-methyl-
p-benzoquinone,5-bis(1-aziridinyl)-3-(2-hydroxy-1-methoxyethyl)-6-methyl-, carbamate (ester)
carbaziloquinone
24279-91-2
mls002703012 ,
2, carbamate ester
carbazilquinone
carbazilequinone
2,4-dione, 2,5-bis(1-aziridinyl)-6 (2-hydroxy-1-methoxyethyl)-3-methyl-, carbamate
nsc-134679
nsc134679
cs 310
p-benzoquinone, 2,5-bis(1-aziridinyl)-3-(2-hydroxy-1-methoxyethyl)-6-methyl-, carbamate (ester)
ccris 2748
carboquona [inn-spanish]
2-(2-((aminocarbonyl)oxy)-1-methoxyethyl)-3,6-bis(1-aziridinyl)-5-methyl-2,5-cyclohexadiene-1,4-dione
nsc 134679
2,5-bis(1-aziridinyl)-3-(2-carbamoyloxy-1-methoxyethyl)-6-methyl-1,4-benzoquinone
carboquonum [inn-latin]
2,5-bis(1-aziridinyl)-3-(2-hydroxy-1-methoxyethyl)-6-methyl-p-benzoquinone carbamate (ester)
2,5-cyclohexadiene-1,4-dione, 2-(2-((aminocarbonyl)oxy)-1-methoxyethyl)-3,6-bis(1-aziridinyl)-5-methyl-
carboquone [inn:jan]
brn 1400765
NCGC00181140-01
[2-[2,5-bis(aziridin-1-yl)-4-methyl-3,6-dioxo-cyclohexa-1,4-dien-1-yl]-2-methoxy-ethyl] carbamate
2,5-bis(1-aziridinyl)-3-(2-hydroxy-1- methoxyethyl)-6-methyl-1,4-benzoquinone, carbamate (ester)
esquinon
carboquone
carboquone (jan/inn)
esquinon (tn)
D01270
NCI60_000771
[2-[2,5-bis(aziridin-1-yl)-4-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl]-2-methoxyethyl] carbamate
cas-24279-91-2
dtxsid8046870 ,
tox21_112746
dtxcid6026870
1cb0hbt12c ,
carboquonum
carboquona
5-20-01-00076 (beilstein handbook reference)
unii-1cb0hbt12c
SCHEMBL8079
carboquone [who-dd]
carboquone [jan]
carboquone [mi]
carboquone [mart.]
carboquone [inn]
CHEBI:31356
Q5038065
DB13677
2-(2,5-di(aziridin-1-yl)-4-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl)-2-methoxyethyl carbamate

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
"A striking chemotherapeutically curative effect on tumor was obtained by means of temporary interruption of regional blood flow combined with local hyperthermia."( Temporary interruption of regional blood flow combined with local hyperthermia for cancer chemotherapy.
Aoki, K; Baba, T; Kanematsu, T; Kidera, Y; Kimura, M, 1976
)
0.26
" During the past eleven years, we have used postoperative chemotherapy in three ways over three different periods: in the earliest period, short-term combined chemotherapy (STCC) was used, in the middle period, intermittent long-term combined chemotherapy (ILTCC) was used in combination with immunotherapy for a randomized group, and in the latest period, when continuous long-term combined chemotherapy (CLTCC) with immunotherapy was employed."( [Clinical value of postoperative chemotherapy for non-small cell lung cancer--with special reference to long-term combined chemotherapy combined with immunotherapy].
Hashizume, Y; Ichihashi, T; Iida, S; Kimoto, H; Kobayashi, H; Sato, H; Shimizu, J; Tsunamura, Y; Watanabe, Y; Yamada, T, 1985
)
0.27
" Thus, hyperthermochemotherapy using CQ combined with HYD, seems to selectively attack a solid tumor."( Hydralazine combined with hyperthermia enhances the effects of carboquone.
Baba, H; Emi, Y; Kusumoto, T; Maehara, Y; Sugimachi, K; Takahashi, I; Yoshida, M,
)
0.13

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Drug dose-response and time-response curves were plotted, and the IC50 ratio was calculated, for each test compound in order to investigate the mechanism of anticancer action."( [In vitro sensitivity test of a cultured human ovarian cancer cell line to anticancer agents].
Fujiya, S; Hatiya, S; Nakabayashi, Y; Tahira, K; Terashima, Y; Yasuda, M; Yoshioka, M, 1985
)
0.27
" Long-term daily administration was shown to be more effective than intermittent dosage in the treatment of Lewis lung carcinoma."( [Antitumor effect of FU-O-G, new antitumor agent, following long term administration].
Arakawa, M; Inomata, T; Mizuno, H; Shimizu, F; Umezawa, T, 1984
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organic molecular entityAny molecular entity that contains carbon.
[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 (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency50.11870.100020.879379.4328AID588453
USP1 protein, partialHomo sapiens (human)Potency25.11890.031637.5844354.8130AID743255
TDP1 proteinHomo sapiens (human)Potency0.08970.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency8.77920.000221.22318,912.5098AID743035; AID743036; AID743042; AID743053; AID743054
Smad3Homo sapiens (human)Potency10.00000.00527.809829.0929AID588855
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency4.25270.000214.376460.0339AID720691; AID720692
estrogen nuclear receptor alphaHomo sapiens (human)Potency4.71270.000229.305416,493.5996AID743069; AID743075; AID743078; AID743079; AID743080; AID743091
67.9K proteinVaccinia virusPotency2.03860.00018.4406100.0000AID720579; AID720580
IDH1Homo sapiens (human)Potency6.51310.005210.865235.4813AID686970
aryl hydrocarbon receptorHomo sapiens (human)Potency29.84930.000723.06741,258.9301AID743085; AID743122
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency21.13170.001723.839378.1014AID743083
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency2.51190.10009.191631.6228AID1346983
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency1.05880.00419.984825.9290AID504444; AID720524
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency0.16790.000323.4451159.6830AID743065; AID743067
importin subunit beta-1 isoform 1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
snurportin-1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency28.18380.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency1.13900.004611.374133.4983AID624296; AID624297
Glycoprotein hormones alpha chainHomo sapiens (human)Potency3.98114.46688.344810.0000AID624291
Cellular tumor antigen p53Homo sapiens (human)Potency0.31670.002319.595674.0614AID651631; AID720552
Guanine nucleotide-binding protein GHomo sapiens (human)Potency8.91251.995325.532750.1187AID624287
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (141)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of cell population proliferationGlycoprotein hormones alpha chainHomo sapiens (human)
hormone-mediated signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
regulation of signaling receptor activityGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of steroid biosynthetic processGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of cell migrationGlycoprotein hormones alpha chainHomo sapiens (human)
thyroid gland developmentGlycoprotein hormones alpha chainHomo sapiens (human)
luteinizing hormone secretionGlycoprotein hormones alpha chainHomo sapiens (human)
organ growthGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlycoprotein hormones alpha chainHomo sapiens (human)
negative regulation of organ growthGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone secretionGlycoprotein hormones alpha chainHomo sapiens (human)
thyroid hormone generationGlycoprotein hormones alpha chainHomo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (38)

Processvia Protein(s)Taxonomy
hormone activityGlycoprotein hormones alpha chainHomo sapiens (human)
protein bindingGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone activityGlycoprotein hormones alpha chainHomo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
extracellular regionGlycoprotein hormones alpha chainHomo sapiens (human)
extracellular spaceGlycoprotein hormones alpha chainHomo sapiens (human)
Golgi lumenGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone complexGlycoprotein hormones alpha chainHomo sapiens (human)
pituitary gonadotropin complexGlycoprotein hormones alpha chainHomo sapiens (human)
extracellular spaceGlycoprotein hormones alpha chainHomo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (39)

Assay IDTitleYearJournalArticle
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.
AID1130143Antileukemic activity against mouse L1210 cells allografted in BDF1 mouse assessed as concentration required to give maximum increase in life span administered for 1 day1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Quantitative structure-activity relationships in 2,5-bis(1-aziridinyl)-p-benzoquinone derivatives against leukemia L-1210.
AID72099log 1/MIC for fungi in mmol/L1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID21056Electrochemically observed pKa (pKred) of aziridines1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID132974Minimum Effective Dose (MED) which cause 40% increase in life span, after singular injection at log (1/C).1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
AID133615Optimal Dose (OD) which cause maximum increase in the life span, after chronic injection at log (1/C).1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
AID97908log 1/D125 for the dose (mmol/kg) to give 125%T/C ratio (L1210) in vivo1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID1130142Antileukemic activity against mouse L1210 cells allografted in BDF1 mouse assessed as concentration required to increase 40% life span administered for 1 day1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Quantitative structure-activity relationships in 2,5-bis(1-aziridinyl)-p-benzoquinone derivatives against leukemia L-1210.
AID55494DNA cross link ratio at pH=5.0 and 50 umol/L compound1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID228716log 1/anion production.1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID1130144Antileukemic activity against mouse L1210 cells allografted in BDF1 mouse assessed as concentration required to increase 40% life span administered as continuous injection1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Quantitative structure-activity relationships in 2,5-bis(1-aziridinyl)-p-benzoquinone derivatives against leukemia L-1210.
AID228715log 1/LD50 for LD50 (mmol/kg)1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID97909log 1/ID75 for the in vitro clonogenic L1210 assay with ID75 in umol/L1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID1130141Antileukemic activity against mouse L1210 cells allografted in BDF1 mouse assessed as concentration required to give maximum increase in life span administered as qd for 12 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Quantitative structure-activity relationships in 2,5-bis(1-aziridinyl)-p-benzoquinone derivatives against leukemia L-1210.
AID132973Minimum Effective Dose (MED) which cause 40% increase in life span, after chronic injection at log (1/C).1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
AID228714log KGSH for the rate k of glutathione (GSH) consumption in 1/s1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID19426HPLC capacity factor (logK)1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID37613log 1/D125 or the dose (mmol/kg) to give 125%T/C ratio (B16) in vivo1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID19922E1/2 for the half-wave potential at pH=7.0 in V571996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID18769Observed rate of hydrolysis (logKobs) (pH=4.0)1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID133616Optimal Dose (OD) which cause maximum increase in the life span, after singular injection at log (1/C).1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
AID1130146Chemotherapeutic index, ratio of antileukemic activity against mouse L1210 cells allografted in BDF1 mouse assessed as concentration required to give maximum increase in life span administered as continuous injection to antileukemic activity against mouse1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Quantitative structure-activity relationships in 2,5-bis(1-aziridinyl)-p-benzoquinone derivatives against leukemia L-1210.
AID19838Partition coefficient (logP)1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
In vivo activity and hydrophobicity of cytostatic aziridinyl quinones.
AID1130140Antileukemic activity against mouse L1210 cells allografted in BDF1 mouse assessed as concentration required to increase 40% life span administered as qd for 12 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Quantitative structure-activity relationships in 2,5-bis(1-aziridinyl)-p-benzoquinone derivatives against leukemia L-1210.
AID1130145Antileukemic activity against mouse L1210 cells allografted in BDF1 mouse assessed as concentration required to give maximum increase in life span administered as continuous injection1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Quantitative structure-activity relationships in 2,5-bis(1-aziridinyl)-p-benzoquinone derivatives against leukemia L-1210.
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.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (186)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990135 (72.58)18.7374
1990's38 (20.43)18.2507
2000's7 (3.76)29.6817
2010's4 (2.15)24.3611
2020's2 (1.08)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.63

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index8.63 (24.57)
Research Supply Index5.36 (2.92)
Research Growth Index3.99 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.63)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (8.16%)5.53%
Reviews6 (3.06%)6.00%
Case Studies27 (13.78%)4.05%
Observational0 (0.00%)0.25%
Other147 (75.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]