Page last updated: 2024-10-15

apogossypolone

Description

apogossypolone: has antineoplastic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135513044
CHEMBL ID1272170
SCHEMBL ID1890983
MeSH IDM0528589

Synonyms (20)

Synonym
CHEMBL1272170 ,
SCHEMBL1890983
2-(6,7-dihydroxy-5-isopropyl-3-methyl-1,4-dioxo-2-naphthyl)-6,7-dihydroxy-5-isopropyl-3-methyl-naphthalene-1,4-dione
apogossypolone
GYYXKPBLWDDQQK-UHFFFAOYSA-N
6,6',7,7'-tetrahydroxy-5,5'-diisopropyl-3,3'-dimethyl-2,2'-binaphthyl-1,1',4,4'-tetraone
bdbm142745
us8937193, 6a
886578-07-0
6,6',7,7'-tetrahydroxy-5,5'-diisopropyl-3,3'-dimethyl-[2,2'-binaphthalene]-1,1',4,4'-tetraone
DTXSID40469551
JOVVKPCDUDNVPP-UHFFFAOYSA-N
A917663
6-(1,4-dihydroxy-3-methyl-6,7-dioxo-5-propan-2-ylnaphthalen-2-yl)-5,8-dihydroxy-7-methyl-1-propan-2-ylnaphthalene-2,3-dione
6,7,6',7'-tetrahydroxy-5,5'-diisopropyl-3,3'-dimethyl-[2,2']binaphthalenyl-1,4,1',4'-tetraone
6,6',7,7'-tetrahydroxy-3,3'-dimethyl-5,5'-bis(1-methylethyl)-[2,2'-binaphthalene]-1,1',4,4'-tetrone
3-methyl-5-propan-2-yl-2-(1,4,6,7-tetrahydroxy-3-methyl-5-propan-2-ylnaphthalen-2-yl)naphthalene-1,4,6,7-tetrone
CS-0015647
HY-19551
PD118228

Research Excerpts

Overview

Apogossypolone (ApoG2) is an analogue of (-)-gossypols. It functions as a potent pan-Bcl-2 family inhibitor. It seems therapeutically promising for future translational studies.

ExcerptReference
"apogossypolone (ApoG2) is a novel derivate of gossypol. "( ApoG2 induces cell cycle arrest of nasopharyngeal carcinoma cells by suppressing the c-Myc signaling pathway.
Hu, ZY; Sun, J; Yang, D; Zeng, YX; Zhu, XF, 2009
)
"Apogossypolone (ApoG2) is an analogue of (-)-gossypol, exhibiting binding activity with Ki values of 35 nmol/L for Bcl-2 and 25 nmol/L for Mcl-1."( Preclinical studies of apogossypolone, a novel pan inhibitor of bcl-2 and mcl-1, synergistically potentiates cytotoxic effect of gemcitabine in pancreatic cancer cells.
Aboukameel, A; Banerjee, S; Chen, J; Choi, M; Mohammad, M; Mohammad, RM; Sarkar, FH; Wang, Z; Yang, D, 2010
)
"Apogossypolone, which functions as a potent pan-Bcl-2 family inhibitor, seems therapeutically promising for future translational studies including the treatment of pancreatic cancer."( Preclinical studies of apogossypolone, a novel pan inhibitor of bcl-2 and mcl-1, synergistically potentiates cytotoxic effect of gemcitabine in pancreatic cancer cells.
Aboukameel, A; Banerjee, S; Chen, J; Choi, M; Mohammad, M; Mohammad, RM; Sarkar, FH; Wang, Z; Yang, D, 2010
)

Dosage Studied

ExcerptReference
" One-fifth normal dosage of the two drugs in MLDC NCs exhibited significantly higher anti-tumor efficiency in reducing tumor size compared with free drugs combination or single drug-loaded nanoparticles individually, indicating that the mulberry-like dual-drug nanoplatform has a great potential in tumor therapy."( Mulberry-like dual-drug complicated nanocarriers assembled with apogossypolone amphiphilic starch micelles and doxorubicin hyaluronic acid nanoparticles for tumor combination and targeted therapy.
Chen, M; Gao, W; Li, K; Liu, H; Liu, J; Wu, D; Xu, L; Zeng, Y, 2015
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Apoptosis regulator Bcl-2Homo sapiens (human)IC50 (µMol)0.37000.00100.57634.3000AID528395
Apoptosis regulator Bcl-2Homo sapiens (human)Ki0.10670.00000.19012.9000AID1599462; AID1858780; AID528395
BH3-interacting domain death agonistHomo sapiens (human)IC50 (µMol)0.34250.02501.08673.0300AID1858754; AID1858796
Bcl-2-like protein 1Homo sapiens (human)IC50 (µMol)0.64500.00031.04829.5400AID1858796; AID528394
Bcl-2-like protein 1Homo sapiens (human)Ki0.58000.00000.45819.0000AID1599463; AID1858779; AID528394
Induced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)IC50 (µMol)0.28250.00442.923510.0000AID1858754; AID528397
Induced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)Ki8.48500.00101.46539.5400AID1599464; AID1858781; AID528397
Bcl-2-related protein A1Homo sapiens (human)IC50 (µMol)2.17000.00441.65144.3000AID528396
Bcl-2-related protein A1Homo sapiens (human)Ki1.47001.47003.40005.3300AID528396
[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)
Bcl-2-like protein 1Homo sapiens (human)Kd2.80000.00010.90252.8000AID528398
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (176)

Processvia Protein(s)Taxonomy
protein polyubiquitinationApoptosis regulator Bcl-2Homo sapiens (human)
apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsApoptosis regulator Bcl-2Homo sapiens (human)
response to xenobiotic stimulusApoptosis regulator Bcl-2Homo sapiens (human)
response to toxic substanceApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of cell growthApoptosis regulator Bcl-2Homo sapiens (human)
response to cytokineApoptosis regulator Bcl-2Homo sapiens (human)
B cell proliferationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
regulation of calcium ion transportApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandApoptosis regulator Bcl-2Homo sapiens (human)
G1/S transition of mitotic cell cycleApoptosis regulator Bcl-2Homo sapiens (human)
ossificationApoptosis regulator Bcl-2Homo sapiens (human)
ovarian follicle developmentApoptosis regulator Bcl-2Homo sapiens (human)
metanephros developmentApoptosis regulator Bcl-2Homo sapiens (human)
branching involved in ureteric bud morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
behavioral fear responseApoptosis regulator Bcl-2Homo sapiens (human)
B cell homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
B cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
release of cytochrome c from mitochondriaApoptosis regulator Bcl-2Homo sapiens (human)
regulation of cell-matrix adhesionApoptosis regulator Bcl-2Homo sapiens (human)
lymphoid progenitor cell differentiationApoptosis regulator Bcl-2Homo sapiens (human)
B cell lineage commitmentApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of B cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
response to ischemiaApoptosis regulator Bcl-2Homo sapiens (human)
renal system processApoptosis regulator Bcl-2Homo sapiens (human)
melanin metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
regulation of nitrogen utilizationApoptosis regulator Bcl-2Homo sapiens (human)
autophagyApoptosis regulator Bcl-2Homo sapiens (human)
humoral immune responseApoptosis regulator Bcl-2Homo sapiens (human)
DNA damage responseApoptosis regulator Bcl-2Homo sapiens (human)
actin filament organizationApoptosis regulator Bcl-2Homo sapiens (human)
axonogenesisApoptosis regulator Bcl-2Homo sapiens (human)
female pregnancyApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of cell population proliferationApoptosis regulator Bcl-2Homo sapiens (human)
male gonad developmentApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressApoptosis regulator Bcl-2Homo sapiens (human)
response to radiationApoptosis regulator Bcl-2Homo sapiens (human)
response to xenobiotic stimulusApoptosis regulator Bcl-2Homo sapiens (human)
response to toxic substanceApoptosis regulator Bcl-2Homo sapiens (human)
post-embryonic developmentApoptosis regulator Bcl-2Homo sapiens (human)
response to iron ionApoptosis regulator Bcl-2Homo sapiens (human)
response to UV-BApoptosis regulator Bcl-2Homo sapiens (human)
response to gamma radiationApoptosis regulator Bcl-2Homo sapiens (human)
regulation of gene expressionApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of autophagyApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of calcium ion transport into cytosolApoptosis regulator Bcl-2Homo sapiens (human)
regulation of glycoprotein biosynthetic processApoptosis regulator Bcl-2Homo sapiens (human)
mesenchymal cell developmentApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of neuron maturationApoptosis regulator Bcl-2Homo sapiens (human)
smooth muscle cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of smooth muscle cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
cochlear nucleus developmentApoptosis regulator Bcl-2Homo sapiens (human)
gland morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
regulation of transmembrane transporter activityApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of ossificationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cell growthApoptosis regulator Bcl-2Homo sapiens (human)
melanocyte differentiationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of B cell proliferationApoptosis regulator Bcl-2Homo sapiens (human)
hair follicle morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
axon regenerationApoptosis regulator Bcl-2Homo sapiens (human)
regulation of protein stabilityApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulum calcium ion homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
glomerulus developmentApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cellular pH reductionApoptosis regulator Bcl-2Homo sapiens (human)
regulation of protein localizationApoptosis regulator Bcl-2Homo sapiens (human)
myeloid cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of myeloid cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
T cell differentiation in thymusApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationApoptosis regulator Bcl-2Homo sapiens (human)
osteoblast proliferationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of osteoblast proliferationApoptosis regulator Bcl-2Homo sapiens (human)
response to nicotineApoptosis regulator Bcl-2Homo sapiens (human)
organ growthApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of multicellular organism growthApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to glucose starvationApoptosis regulator Bcl-2Homo sapiens (human)
response to hydrogen peroxideApoptosis regulator Bcl-2Homo sapiens (human)
neuron maturationApoptosis regulator Bcl-2Homo sapiens (human)
T cell homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
CD8-positive, alpha-beta T cell lineage commitmentApoptosis regulator Bcl-2Homo sapiens (human)
ear developmentApoptosis regulator Bcl-2Homo sapiens (human)
regulation of viral genome replicationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of melanocyte differentiationApoptosis regulator Bcl-2Homo sapiens (human)
retinal cell programmed cell deathApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of retinal cell programmed cell deathApoptosis regulator Bcl-2Homo sapiens (human)
regulation of mitochondrial membrane permeabilityApoptosis regulator Bcl-2Homo sapiens (human)
focal adhesion assemblyApoptosis regulator Bcl-2Homo sapiens (human)
spleen developmentApoptosis regulator Bcl-2Homo sapiens (human)
thymus developmentApoptosis regulator Bcl-2Homo sapiens (human)
digestive tract morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
oocyte developmentApoptosis regulator Bcl-2Homo sapiens (human)
skeletal muscle fiber developmentApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of skeletal muscle fiber developmentApoptosis regulator Bcl-2Homo sapiens (human)
pigment granule organizationApoptosis regulator Bcl-2Homo sapiens (human)
stem cell developmentApoptosis regulator Bcl-2Homo sapiens (human)
homeostasis of number of cells within a tissueApoptosis regulator Bcl-2Homo sapiens (human)
B cell receptor signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
response to glucocorticoidApoptosis regulator Bcl-2Homo sapiens (human)
neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
defense response to virusApoptosis regulator Bcl-2Homo sapiens (human)
establishment of localization in cellApoptosis regulator Bcl-2Homo sapiens (human)
regulation of mitochondrial membrane potentialApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of mitochondrial depolarizationApoptosis regulator Bcl-2Homo sapiens (human)
hematopoietic stem cell differentiationApoptosis regulator Bcl-2Homo sapiens (human)
calcium ion transport into cytosolApoptosis regulator Bcl-2Homo sapiens (human)
T cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of T cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to organic substanceApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to hypoxiaApoptosis regulator Bcl-2Homo sapiens (human)
reactive oxygen species metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
dendritic cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
motor neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
cell-cell adhesionApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorApoptosis regulator Bcl-2Homo sapiens (human)
epithelial cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of epithelial cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of G1/S transition of mitotic cell cycleApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of dendritic cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of motor neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of anoikisApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageApoptosis regulator Bcl-2Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandApoptosis regulator Bcl-2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
release of cytochrome c from mitochondriaBH3-interacting domain death agonistHomo sapiens (human)
protein targeting to mitochondrionBH3-interacting domain death agonistHomo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsBH3-interacting domain death agonistHomo sapiens (human)
positive regulation of mitochondrial membrane potentialBH3-interacting domain death agonistHomo sapiens (human)
positive regulation of protein-containing complex assemblyBH3-interacting domain death agonistHomo sapiens (human)
regulation of T cell proliferationBH3-interacting domain death agonistHomo sapiens (human)
signal transduction in response to DNA damageBH3-interacting domain death agonistHomo sapiens (human)
mitochondrial ATP synthesis coupled electron transportBH3-interacting domain death agonistHomo sapiens (human)
positive regulation of apoptotic processBH3-interacting domain death agonistHomo sapiens (human)
regulation of epithelial cell proliferationBH3-interacting domain death agonistHomo sapiens (human)
neuron apoptotic processBH3-interacting domain death agonistHomo sapiens (human)
protein-containing complex assemblyBH3-interacting domain death agonistHomo sapiens (human)
establishment of protein localization to membraneBH3-interacting domain death agonistHomo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaBH3-interacting domain death agonistHomo sapiens (human)
hepatocyte apoptotic processBH3-interacting domain death agonistHomo sapiens (human)
mitochondrial outer membrane permeabilizationBH3-interacting domain death agonistHomo sapiens (human)
supramolecular fiber organizationBH3-interacting domain death agonistHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damageBH3-interacting domain death agonistHomo sapiens (human)
regulation of G1/S transition of mitotic cell cycleBH3-interacting domain death agonistHomo sapiens (human)
positive regulation of fibroblast apoptotic processBH3-interacting domain death agonistHomo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathwayBH3-interacting domain death agonistHomo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayBH3-interacting domain death agonistHomo sapiens (human)
apoptotic mitochondrial changesBH3-interacting domain death agonistHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processBH3-interacting domain death agonistHomo sapiens (human)
response to cytokineBcl-2-like protein 1Homo sapiens (human)
negative regulation of apoptotic processBcl-2-like protein 1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptorsBcl-2-like protein 1Homo sapiens (human)
ovarian follicle developmentBcl-2-like protein 1Homo sapiens (human)
in utero embryonic developmentBcl-2-like protein 1Homo sapiens (human)
release of cytochrome c from mitochondriaBcl-2-like protein 1Homo sapiens (human)
endocytosisBcl-2-like protein 1Homo sapiens (human)
germ cell developmentBcl-2-like protein 1Homo sapiens (human)
spermatogenesisBcl-2-like protein 1Homo sapiens (human)
male gonad developmentBcl-2-like protein 1Homo sapiens (human)
apoptotic mitochondrial changesBcl-2-like protein 1Homo sapiens (human)
fertilizationBcl-2-like protein 1Homo sapiens (human)
regulation of cytokinesisBcl-2-like protein 1Homo sapiens (human)
positive regulation of mononuclear cell proliferationBcl-2-like protein 1Homo sapiens (human)
ectopic germ cell programmed cell deathBcl-2-like protein 1Homo sapiens (human)
regulation of growthBcl-2-like protein 1Homo sapiens (human)
negative regulation of apoptotic processBcl-2-like protein 1Homo sapiens (human)
negative regulation of neuron apoptotic processBcl-2-like protein 1Homo sapiens (human)
dendritic cell proliferationBcl-2-like protein 1Homo sapiens (human)
response to cycloheximideBcl-2-like protein 1Homo sapiens (human)
regulation of mitochondrial membrane permeabilityBcl-2-like protein 1Homo sapiens (human)
epithelial cell proliferationBcl-2-like protein 1Homo sapiens (human)
negative regulation of developmental processBcl-2-like protein 1Homo sapiens (human)
neuron apoptotic processBcl-2-like protein 1Homo sapiens (human)
defense response to virusBcl-2-like protein 1Homo sapiens (human)
regulation of mitochondrial membrane potentialBcl-2-like protein 1Homo sapiens (human)
cellular response to amino acid stimulusBcl-2-like protein 1Homo sapiens (human)
cellular response to alkaloidBcl-2-like protein 1Homo sapiens (human)
cellular response to gamma radiationBcl-2-like protein 1Homo sapiens (human)
apoptotic process in bone marrow cellBcl-2-like protein 1Homo sapiens (human)
negative regulation of release of cytochrome c from mitochondriaBcl-2-like protein 1Homo sapiens (human)
dendritic cell apoptotic processBcl-2-like protein 1Homo sapiens (human)
hepatocyte apoptotic processBcl-2-like protein 1Homo sapiens (human)
negative regulation of execution phase of apoptosisBcl-2-like protein 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damageBcl-2-like protein 1Homo sapiens (human)
negative regulation of endoplasmic reticulum stress-induced intrinsic apoptotic signaling pathwayBcl-2-like protein 1Homo sapiens (human)
negative regulation of protein localization to plasma membraneBcl-2-like protein 1Homo sapiens (human)
negative regulation of reproductive processBcl-2-like protein 1Homo sapiens (human)
negative regulation of dendritic cell apoptotic processBcl-2-like protein 1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandBcl-2-like protein 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayBcl-2-like protein 1Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageBcl-2-like protein 1Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandBcl-2-like protein 1Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processBcl-2-like protein 1Homo sapiens (human)
DNA damage responseInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
response to cytokineInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cell fate determinationInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of autophagyInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cellular homeostasisInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
positive regulation of apoptotic processInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of apoptotic processInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
protein transmembrane transportInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
positive regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathwayInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of anoikisInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrial fusionInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
release of cytochrome c from mitochondriaInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of apoptotic processBcl-2-related protein A1Homo sapiens (human)
transmembrane transportBcl-2-related protein A1Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageBcl-2-related protein A1Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processBcl-2-related protein A1Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandBcl-2-related protein A1Homo sapiens (human)
release of cytochrome c from mitochondriaBcl-2-related protein A1Homo sapiens (human)
mitochondrial fusionBcl-2-related protein A1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
protease bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein bindingApoptosis regulator Bcl-2Homo sapiens (human)
channel activityApoptosis regulator Bcl-2Homo sapiens (human)
channel inhibitor activityApoptosis regulator Bcl-2Homo sapiens (human)
ubiquitin protein ligase bindingApoptosis regulator Bcl-2Homo sapiens (human)
identical protein bindingApoptosis regulator Bcl-2Homo sapiens (human)
sequence-specific DNA bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein heterodimerization activityApoptosis regulator Bcl-2Homo sapiens (human)
BH3 domain bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein phosphatase 2A bindingApoptosis regulator Bcl-2Homo sapiens (human)
molecular adaptor activityApoptosis regulator Bcl-2Homo sapiens (human)
DNA-binding transcription factor bindingApoptosis regulator Bcl-2Homo sapiens (human)
BH domain bindingApoptosis regulator Bcl-2Homo sapiens (human)
death receptor bindingBH3-interacting domain death agonistHomo sapiens (human)
protein bindingBH3-interacting domain death agonistHomo sapiens (human)
ubiquitin protein ligase bindingBH3-interacting domain death agonistHomo sapiens (human)
protein bindingBcl-2-like protein 1Homo sapiens (human)
protein kinase bindingBcl-2-like protein 1Homo sapiens (human)
identical protein bindingBcl-2-like protein 1Homo sapiens (human)
BH3 domain bindingBcl-2-like protein 1Homo sapiens (human)
BH domain bindingBcl-2-like protein 1Homo sapiens (human)
protein bindingInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
protein transmembrane transporter activityInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
protein heterodimerization activityInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
BH3 domain bindingInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
channel activityInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
BH domain bindingInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
protein bindingBcl-2-related protein A1Homo sapiens (human)
channel activityBcl-2-related protein A1Homo sapiens (human)
BH domain bindingBcl-2-related protein A1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
mitochondrial outer membraneApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulum membraneApoptosis regulator Bcl-2Homo sapiens (human)
nucleusApoptosis regulator Bcl-2Homo sapiens (human)
cytoplasmApoptosis regulator Bcl-2Homo sapiens (human)
mitochondrionApoptosis regulator Bcl-2Homo sapiens (human)
mitochondrial outer membraneApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulumApoptosis regulator Bcl-2Homo sapiens (human)
cytosolApoptosis regulator Bcl-2Homo sapiens (human)
membraneApoptosis regulator Bcl-2Homo sapiens (human)
nuclear membraneApoptosis regulator Bcl-2Homo sapiens (human)
myelin sheathApoptosis regulator Bcl-2Homo sapiens (human)
BAD-BCL-2 complexApoptosis regulator Bcl-2Homo sapiens (human)
protein-containing complexApoptosis regulator Bcl-2Homo sapiens (human)
pore complexApoptosis regulator Bcl-2Homo sapiens (human)
mitochondrial outer membraneBH3-interacting domain death agonistHomo sapiens (human)
cytosolBH3-interacting domain death agonistHomo sapiens (human)
membraneBH3-interacting domain death agonistHomo sapiens (human)
mitochondrionBH3-interacting domain death agonistHomo sapiens (human)
cytosolBH3-interacting domain death agonistHomo sapiens (human)
cytoplasmBcl-2-like protein 1Homo sapiens (human)
mitochondrionBcl-2-like protein 1Homo sapiens (human)
mitochondrial outer membraneBcl-2-like protein 1Homo sapiens (human)
mitochondrial inner membraneBcl-2-like protein 1Homo sapiens (human)
mitochondrial matrixBcl-2-like protein 1Homo sapiens (human)
endoplasmic reticulumBcl-2-like protein 1Homo sapiens (human)
centrosomeBcl-2-like protein 1Homo sapiens (human)
cytosolBcl-2-like protein 1Homo sapiens (human)
synaptic vesicle membraneBcl-2-like protein 1Homo sapiens (human)
nuclear membraneBcl-2-like protein 1Homo sapiens (human)
Bcl-2 family protein complexBcl-2-like protein 1Homo sapiens (human)
mitochondrial outer membraneBcl-2-like protein 1Homo sapiens (human)
nucleusInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
nucleoplasmInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cytoplasmInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrionInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrial outer membraneInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cytosolInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
membraneInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
Bcl-2 family protein complexInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrial outer membraneInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cytoplasmBcl-2-related protein A1Homo sapiens (human)
cytosolBcl-2-related protein A1Homo sapiens (human)
mitochondrial outer membraneBcl-2-related protein A1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (32)

Assay IDTitleYearJournalArticle
AID528390Cytotoxicity against human H460 cells expressing high level of Bcl-2 after 72 hrs by ATP-LITE assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID1858780Binding affinity to Bcl-2 (unknown origin)2021European journal of medicinal chemistry, Jan-15, Volume: 210Development of Mcl-1 inhibitors for cancer therapy.
AID528398Binding affinity Bcl-xL by isothermal titration calorimetry assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528394Displacement of F-BakBH3 from Bcl-xL after 30 mins by fluorescence polarization assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528414Toxicity in human PPC1 cells xenografted nude mouse assessed as weight loss at 50 mg/kg, ip administered weekly 3 times2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528406Reduction of spleen weight in human Bcl2 expressing B6 transgenic BALB/c mouse at 60 umol/kg, ip administered as single dose after 24 hrs2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID1858754Inhibition of Mcl-1/Bid (unknown origin) by fluorescence polarization assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Development of Mcl-1 inhibitors for cancer therapy.
AID528405Induction of apoptosis in human CLL after 24 hrs by annexin V-FITC and propidium iodide staining2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528399Metabolic stability of the compound in rat plasma after 40 mins2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528396Displacement of F-BakBH3 from Bfl-1 after 30 mins by fluorescence polarization assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID1599464Inhibition of Flu-BakBH3 peptide binding to recombinant human MCL1 after 15 mins by fluorescence polarization assay2019European journal of medicinal chemistry, Sep-01, Volume: 177The chemical biology of apoptosis: Revisited after 17 years.
AID1858779Binding affinity to Bcl-XL (unknown origin)2021European journal of medicinal chemistry, Jan-15, Volume: 210Development of Mcl-1 inhibitors for cancer therapy.
AID528389Cytotoxicity against human PC3 cells expressing high level of Bcl-xL after 72 hrs by ATP-LITE assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528404Reduction of spleen weight in ip dosed human Bcl2 expressing B6 transgenic BALB/c mouse administered as single dose after 24 hrs2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528395Displacement of F-BakBH3 from Bcl-2 after 30 mins by fluorescence polarization assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID1599463Inhibition of Flu-BakBH3 peptide binding to recombinant human Bcl-xL after 15 mins by fluorescence polarization assay2019European journal of medicinal chemistry, Sep-01, Volume: 177The chemical biology of apoptosis: Revisited after 17 years.
AID528403Induction of apoptosis in human RS4:11 cells expressing high level of Bcl-2 and Bcl-xL after 24 hrs by annexin V-FITC and propidium iodide staining2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528397Displacement of F-BakBH3 from Mcl-1 after 30 mins by fluorescence polarization assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528388Binding affinity Bcl-xL at 200 uM by one-dimensional 1H nuclear magnetic resonance spectroscopy2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID1599462Inhibition of Flu-BakBH3 peptide binding to recombinant human Bcl2 after 15 mins by fluorescence polarization assay2019European journal of medicinal chemistry, Sep-01, Volume: 177The chemical biology of apoptosis: Revisited after 17 years.
AID528402Induction of apoptosis in human BP3 cells expressing high level of Bfl-1 and Mcl-1 after 24 hrs by annexin V-FITC and propidium iodide staining2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528391Cytotoxicity against human H1299 cells expressing high level of Mcl-1 after 72 hrs by ATP-LITE assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID1858796Inhibition of Bcl-xL/Bid (unknown origin) by fluorescence polarization assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Development of Mcl-1 inhibitors for cancer therapy.
AID528393Cytotoxicity against human RS4:11 cells expressing high level of Bcl-2 and Bcl-xL after 72 hrs by annexin V-FITC and propidium iodide staining2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528417Antitumor activity against human PPC1 cells xenografted in nude mouse assessed as tumor regression at 50 mg/kg, ip administered 5 times measured on after 2 weeks relative to control2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528413Antitumor activity against human PPC1 cells xenografted in nude mouse assessed as tumor regression at 50 mg/kg, ip administered weekly 3 times2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID1858781Binding affinity to Mcl-1 (unknown origin)2021European journal of medicinal chemistry, Jan-15, Volume: 210Development of Mcl-1 inhibitors for cancer therapy.
AID528400Metabolic stability of the compound in rat microsomes after 40 mins2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528401Permeability of the compound by PAMPA2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528392Cytotoxicity against human BP3 cells expressing high level of Bfl-1 and Mcl-1 after 72 hrs by annexin V-FITC and propidium iodide staining2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528418Antitumor activity against human PPC1 cells xenografted in nude mouse assessed as tumor regression at 50 mg/kg, ip administered 6 times measured after 3 weeks relative to control2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
AID528387Metabolic stability of the compound in rat plasma assessed as compound degradation after 1 hr2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (16.13)29.6817
2010's25 (80.65)24.3611
2020's1 (3.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (9.68%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other28 (90.32%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]