Compounds > cortistatin a
Page last updated: 2024-11-12

cortistatin a

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Description

cortistatin A: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

cortistatin A : A member of the class of cortistatins that is substituted by hydroxy groups at positions 1 and 2, a dimethylamino group at the 3alpha position and an isoquinolin-7-yl group at the 17 position, with double bonds at the 9-11 and 10-19 positions (the 1R,2R,17beta enantiomer). [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]

Cross-References

ID SourceID
PubMed CID11561907
CHEMBL ID4080906
CHEBI ID67171
SCHEMBL ID12431713
MeSH IDM0524992

Synonyms (25)

Synonym
cortistatin a
cortistatine a
882976-95-6
unii-6vg04xov89
10a,12a-epoxybenzo(4,5)cyclohept(1,2-e)indene-7,8-diol, 9-(dimethylamino)-1,2,3,3a,4,7,8,9,10,11,12,12b-dodecahydro-3-(7-isoquinolinyl)-3a-methyl-, (3s,3ar,7r,8r,9s,10ar,12as,12br)-
6vg04xov89 ,
(3s,3ar,7r,8r,9s,10ar,12as,12br)-9-(dimethylamino)-1,2,3,3a,4,7,8,9,10,11,12,12b-dodecahydro-3-(7-isoquinolinyl)-3a-methyl-10a,12a-epoxybenzo(4,5)cyclohept(1,2-e)indene-7,8-diol
17-epi-cortistatin a
cortistatin a [mi]
(1r,2r,3s,5r,8alpha,17beta)-3-(dimethylamino)-17-(isoquinolin-7-yl)-5,8-epoxy-9,19-cyclo-9,10-secoandrosta-9(11),10-diene-1,2-diol
(+)-cortistatin a
CHEBI:67171
(1r,2r,3s,5r)-3-(dimethylamino)-17beta-(isoquinolin-7-yl)-5,8alpha-epoxy-9,19-cyclo-9,10-secoandrosta-9(11),10-diene-1,2-diol
c1i ,
SCHEMBL12431713
DTXSID10468617
gtpl9885
(1r,2r,3s,5r,17alpha)-3-(dimethylamino)-17-(isoquinolin-7-yl)-5,8-epoxy-9,19-cyclo-9,10-secoandrosta-9(11),10-diene-1,2-diol
bdbm50248631
Q5173335
CHEMBL4080906 ,
(3s,3ar,7r,8r,9s,10ar,12as,12br)-9-(dimethylamino)-3-(isoquinolin-7-yl)-3a-methyl-1,2,3,3a,4,7,8,9,10,11,12,12b-dodecahydro-10a,12a-epoxybenzo[4,5]cyclohepta[1,2-e]indene-7,8-diol
(1s,2r,5s,6r,12r,13r,14s,16r)-14-(dimethylamino)-5-isoquinolin-7-yl-6-methyl-19-oxapentacyclo[14.2.1.01,9.02,6.011,16]nonadeca-8,10-diene-12,13-diol
10a,12a-epoxybenzo[4,5]cyclohept[1,2-e]indene-7,8-diol, 9-(dimethylamino)-1,2,3,3a,4,7,8,9,10,11,12,12b-dodecahydro-3-(7-isoquinolinyl)-3a-methyl-, (3s,3ar,7r,8r,9s,10ar,12as,12br)-
AKOS040745681

Research Excerpts

Overview

Cortistatin A (CA) is a highly selective inhibitor of the Mediator kinases CDK8 and CDK19.

ExcerptReferenceRelevance
"Cortistatin A (CA) is a highly selective inhibitor of the Mediator kinases CDK8 and CDK19. "( Identification of Mediator Kinase Substrates in Human Cells using Cortistatin A and Quantitative Phosphoproteomics.
Dowell, RD; Ebmeier, CC; Lee, T; Odell, AT; Old, WM; Pelish, HE; Poss, ZC; Shair, MD; Taatjes, DJ; Tangpeerachaikul, A, 2016)		2.11

Dosage Studied

ExcerptRelevanceReference
" Individually increasing or decreasing the expression of these transcription factors suppressed AML cell growth, providing evidence that leukaemia cells are sensitive to the dosage of SE-associated genes."( Mediator kinase inhibition further activates super-enhancer-associated genes in AML.
Arefolov, A; Armstrong, SA; Banka, D; Bronson, RT; Caruso, BT; Christie, AL; Da Silva, DH; Du, K; Ebmeier, CC; Fadeyi, O; Jestel, A; Kohl, NE; Krivtsov, AV; Kung, AL; Lemieux, ME; Liau, BB; Myers, AG; Nitulescu, II; Pelish, HE; Poss, ZC; Schneider, EV; Shair, MD; Si, C; Taatjes, DJ; Tangpeerachaikul, A; Zou, G, 2015)		0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (3)

ClassDescription
cortistatinsAny member of a class of steroidal alkaloids obtained from the marine sponge Corticium simplex, with a basic skeleton that is (5R,8beta)-5,8-epoxy-9,19-cyclo-9,10-secoandrostane, bearing a dimethylamino substituent at position 3 and an isoquinolin-7-yl or isoquinolin-7-yl-derived substituent at position 17. They selectively inhibit proliferation of human umbilical vein endothelial cells (HUVECs).
diolA compound that contains two hydroxy groups, generally assumed to be, but not necessarily, alcoholic. Aliphatic diols are also called glycols.
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 (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Rho-associated protein kinase 2Homo sapiens (human)IC50 (µMol)0.22000.00020.578010.0000AID1388659
Cyclin-CHomo sapiens (human)IC50 (µMol)0.00500.00500.67925.9000AID1388656
Cyclin-dependent kinase 8Homo sapiens (human)IC50 (µMol)0.00850.00341.02755.9000AID1388656; AID1474304
Rho-associated protein kinase 1Homo sapiens (human)IC50 (µMol)0.25000.00040.854910.0000AID1388658
Cyclin-dependent kinase 19Homo sapiens (human)IC50 (µMol)0.01000.00500.40852.2000AID1388657
[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)
Rho-associated protein kinase 2Homo sapiens (human)Kd0.22000.00022.710556.0660AID1613748
cAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)Kd3.50000.00392.947923.2450AID1613749
Cyclin-dependent kinase 8Homo sapiens (human)Kd0.01700.00141.29088.0000AID1613744
Rho-associated protein kinase 1Homo sapiens (human)Kd0.25000.00031.755513.4620AID1613747
Cyclin-dependent kinase 19Homo sapiens (human)Kd0.01000.00151.92047.2000AID1613746
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (131)

Processvia Protein(s)Taxonomy
epithelial to mesenchymal transitionRho-associated protein kinase 2Homo sapiens (human)
positive regulation of protein phosphorylationRho-associated protein kinase 2Homo sapiens (human)
response to ischemiaRho-associated protein kinase 2Homo sapiens (human)
aortic valve morphogenesisRho-associated protein kinase 2Homo sapiens (human)
protein phosphorylationRho-associated protein kinase 2Homo sapiens (human)
smooth muscle contractionRho-associated protein kinase 2Homo sapiens (human)
canonical NF-kappaB signal transductionRho-associated protein kinase 2Homo sapiens (human)
positive regulation of endothelial cell migrationRho-associated protein kinase 2Homo sapiens (human)
positive regulation of cardiac muscle hypertrophyRho-associated protein kinase 2Homo sapiens (human)
positive regulation of gene expressionRho-associated protein kinase 2Homo sapiens (human)
negative regulation of gene expressionRho-associated protein kinase 2Homo sapiens (human)
positive regulation of centrosome duplicationRho-associated protein kinase 2Homo sapiens (human)
negative regulation of angiogenesisRho-associated protein kinase 2Homo sapiens (human)
actin cytoskeleton organizationRho-associated protein kinase 2Homo sapiens (human)
regulation of cell adhesionRho-associated protein kinase 2Homo sapiens (human)
positive regulation of cell migrationRho-associated protein kinase 2Homo sapiens (human)
cortical actin cytoskeleton organizationRho-associated protein kinase 2Homo sapiens (human)
regulation of nervous system processRho-associated protein kinase 2Homo sapiens (human)
positive regulation of connective tissue growth factor productionRho-associated protein kinase 2Homo sapiens (human)
regulation of actin cytoskeleton organizationRho-associated protein kinase 2Homo sapiens (human)
negative regulation of myosin-light-chain-phosphatase activityRho-associated protein kinase 2Homo sapiens (human)
regulation of circadian rhythmRho-associated protein kinase 2Homo sapiens (human)
positive regulation of MAPK cascadeRho-associated protein kinase 2Homo sapiens (human)
modulation by host of viral processRho-associated protein kinase 2Homo sapiens (human)
negative regulation of nitric oxide biosynthetic processRho-associated protein kinase 2Homo sapiens (human)
regulation of keratinocyte differentiationRho-associated protein kinase 2Homo sapiens (human)
rhythmic processRho-associated protein kinase 2Homo sapiens (human)
centrosome duplicationRho-associated protein kinase 2Homo sapiens (human)
regulation of stress fiber assemblyRho-associated protein kinase 2Homo sapiens (human)
positive regulation of stress fiber assemblyRho-associated protein kinase 2Homo sapiens (human)
regulation of focal adhesion assemblyRho-associated protein kinase 2Homo sapiens (human)
mRNA destabilizationRho-associated protein kinase 2Homo sapiens (human)
negative regulation of biomineral tissue developmentRho-associated protein kinase 2Homo sapiens (human)
cellular response to testosterone stimulusRho-associated protein kinase 2Homo sapiens (human)
response to transforming growth factor betaRho-associated protein kinase 2Homo sapiens (human)
protein localization to plasma membraneRho-associated protein kinase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionRho-associated protein kinase 2Homo sapiens (human)
blood vessel diameter maintenanceRho-associated protein kinase 2Homo sapiens (human)
regulation of angiotensin-activated signaling pathwayRho-associated protein kinase 2Homo sapiens (human)
negative regulation of protein localization to lysosomeRho-associated protein kinase 2Homo sapiens (human)
regulation of cellular response to hypoxiaRho-associated protein kinase 2Homo sapiens (human)
positive regulation of amyloid-beta formationRho-associated protein kinase 2Homo sapiens (human)
positive regulation of protein localization to early endosomeRho-associated protein kinase 2Homo sapiens (human)
positive regulation of amyloid precursor protein catabolic processRho-associated protein kinase 2Homo sapiens (human)
regulation of establishment of endothelial barrierRho-associated protein kinase 2Homo sapiens (human)
negative regulation of bicellular tight junction assemblyRho-associated protein kinase 2Homo sapiens (human)
cellular response to acetylcholineRho-associated protein kinase 2Homo sapiens (human)
positive regulation of connective tissue replacementRho-associated protein kinase 2Homo sapiens (human)
response to angiotensinRho-associated protein kinase 2Homo sapiens (human)
regulation of establishment of cell polarityRho-associated protein kinase 2Homo sapiens (human)
regulation of cell motilityRho-associated protein kinase 2Homo sapiens (human)
actomyosin structure organizationRho-associated protein kinase 2Homo sapiens (human)
peptidyl-threonine phosphorylationRho-associated protein kinase 2Homo sapiens (human)
mitotic cytokinesisRho-associated protein kinase 2Homo sapiens (human)
embryonic morphogenesisRho-associated protein kinase 2Homo sapiens (human)
regulation of cell junction assemblyRho-associated protein kinase 2Homo sapiens (human)
Rho protein signal transductionRho-associated protein kinase 2Homo sapiens (human)
mesoderm formationcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
neural tube closurecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
regulation of heart ratecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
renal water homeostasiscAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
mRNA processingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein phosphorylationcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein export from nucleuscAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwaycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ioncAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
regulation of macroautophagycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
peptidyl-serine phosphorylationcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cytokine-mediated signaling pathwaycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
positive regulation of insulin secretioncAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
negative regulation of interleukin-2 productioncAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
high-density lipoprotein particle assemblycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cellular response to heatcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
mitochondrial protein catabolic processcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
regulation of osteoblast differentiationcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
positive regulation of gluconeogenesiscAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
negative regulation of smoothened signaling pathwaycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
positive regulation of protein export from nucleuscAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
sperm capacitationcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
positive regulation of calcium-mediated signalingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
regulation of cell cyclecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
regulation of cardiac muscle contractioncAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
regulation of proteasomal protein catabolic processcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cellular response to coldcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
regulation of protein processingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cellular response to glucose stimuluscAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cellular response to parathyroid hormone stimuluscAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cellular response to glucagon stimuluscAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cellular response to epinephrine stimuluscAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductioncAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissioncAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
regulation of cardiac conductioncAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
negative regulation of TORC1 signalingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
negative regulation of glycolytic process through fructose-6-phosphatecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein localization to lipid dropletcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
regulation of bicellular tight junction assemblycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein kinase A signalingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
G0 to G1 transitionCyclin-CHomo sapiens (human)
negative regulation of Notch signaling pathwayCyclin-CHomo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-CHomo sapiens (human)
protein ubiquitinationCyclin-dependent kinase 8Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-dependent kinase 8Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 8Homo sapiens (human)
negative regulation of triglyceride metabolic processCyclin-dependent kinase 8Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 8Homo sapiens (human)
epithelial to mesenchymal transitionRho-associated protein kinase 1Homo sapiens (human)
aortic valve morphogenesisRho-associated protein kinase 1Homo sapiens (human)
apical constrictionRho-associated protein kinase 1Homo sapiens (human)
protein phosphorylationRho-associated protein kinase 1Homo sapiens (human)
smooth muscle contractionRho-associated protein kinase 1Homo sapiens (human)
leukocyte cell-cell adhesionRho-associated protein kinase 1Homo sapiens (human)
signal transductionRho-associated protein kinase 1Homo sapiens (human)
canonical NF-kappaB signal transductionRho-associated protein kinase 1Homo sapiens (human)
Rho protein signal transductionRho-associated protein kinase 1Homo sapiens (human)
positive regulation of autophagyRho-associated protein kinase 1Homo sapiens (human)
positive regulation of cardiac muscle hypertrophyRho-associated protein kinase 1Homo sapiens (human)
positive regulation of gene expressionRho-associated protein kinase 1Homo sapiens (human)
positive regulation of phosphatase activityRho-associated protein kinase 1Homo sapiens (human)
negative regulation of angiogenesisRho-associated protein kinase 1Homo sapiens (human)
peptidyl-serine phosphorylationRho-associated protein kinase 1Homo sapiens (human)
membrane to membrane dockingRho-associated protein kinase 1Homo sapiens (human)
actin cytoskeleton organizationRho-associated protein kinase 1Homo sapiens (human)
regulation of cell adhesionRho-associated protein kinase 1Homo sapiens (human)
regulation of cell migrationRho-associated protein kinase 1Homo sapiens (human)
cortical actin cytoskeleton organizationRho-associated protein kinase 1Homo sapiens (human)
neuron projection developmentRho-associated protein kinase 1Homo sapiens (human)
bleb assemblyRho-associated protein kinase 1Homo sapiens (human)
negative regulation of protein bindingRho-associated protein kinase 1Homo sapiens (human)
regulation of actin cytoskeleton organizationRho-associated protein kinase 1Homo sapiens (human)
positive regulation of dephosphorylationRho-associated protein kinase 1Homo sapiens (human)
negative regulation of myosin-light-chain-phosphatase activityRho-associated protein kinase 1Homo sapiens (human)
negative regulation of phosphorylationRho-associated protein kinase 1Homo sapiens (human)
positive regulation of MAPK cascadeRho-associated protein kinase 1Homo sapiens (human)
regulation of keratinocyte differentiationRho-associated protein kinase 1Homo sapiens (human)
regulation of neuron differentiationRho-associated protein kinase 1Homo sapiens (human)
leukocyte migrationRho-associated protein kinase 1Homo sapiens (human)
leukocyte tethering or rollingRho-associated protein kinase 1Homo sapiens (human)
negative regulation of membrane protein ectodomain proteolysisRho-associated protein kinase 1Homo sapiens (human)
myoblast migrationRho-associated protein kinase 1Homo sapiens (human)
regulation of stress fiber assemblyRho-associated protein kinase 1Homo sapiens (human)
regulation of focal adhesion assemblyRho-associated protein kinase 1Homo sapiens (human)
positive regulation of focal adhesion assemblyRho-associated protein kinase 1Homo sapiens (human)
mRNA destabilizationRho-associated protein kinase 1Homo sapiens (human)
negative regulation of biomineral tissue developmentRho-associated protein kinase 1Homo sapiens (human)
regulation of microtubule cytoskeleton organizationRho-associated protein kinase 1Homo sapiens (human)
response to transforming growth factor betaRho-associated protein kinase 1Homo sapiens (human)
protein localization to plasma membraneRho-associated protein kinase 1Homo sapiens (human)
regulation of synapse maturationRho-associated protein kinase 1Homo sapiens (human)
podocyte cell migrationRho-associated protein kinase 1Homo sapiens (human)
motor neuron apoptotic processRho-associated protein kinase 1Homo sapiens (human)
blood vessel diameter maintenanceRho-associated protein kinase 1Homo sapiens (human)
regulation of angiotensin-activated signaling pathwayRho-associated protein kinase 1Homo sapiens (human)
neuron projection arborizationRho-associated protein kinase 1Homo sapiens (human)
positive regulation of amyloid-beta clearanceRho-associated protein kinase 1Homo sapiens (human)
regulation of synaptic vesicle endocytosisRho-associated protein kinase 1Homo sapiens (human)
negative regulation of amyloid-beta formationRho-associated protein kinase 1Homo sapiens (human)
negative regulation of amyloid precursor protein catabolic processRho-associated protein kinase 1Homo sapiens (human)
regulation of establishment of endothelial barrierRho-associated protein kinase 1Homo sapiens (human)
negative regulation of bicellular tight junction assemblyRho-associated protein kinase 1Homo sapiens (human)
positive regulation of connective tissue replacementRho-associated protein kinase 1Homo sapiens (human)
response to angiotensinRho-associated protein kinase 1Homo sapiens (human)
regulation of establishment of cell polarityRho-associated protein kinase 1Homo sapiens (human)
regulation of cell motilityRho-associated protein kinase 1Homo sapiens (human)
negative regulation of motor neuron apoptotic processRho-associated protein kinase 1Homo sapiens (human)
regulation of cell junction assemblyRho-associated protein kinase 1Homo sapiens (human)
mitotic cytokinesisRho-associated protein kinase 1Homo sapiens (human)
embryonic morphogenesisRho-associated protein kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylationRho-associated protein kinase 1Homo sapiens (human)
actomyosin structure organizationRho-associated protein kinase 1Homo sapiens (human)
positive regulation of apoptotic processCyclin-dependent kinase 19Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 19Homo sapiens (human)
cellular response to lipopolysaccharideCyclin-dependent kinase 19Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 19Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

Processvia Protein(s)Taxonomy
protease bindingRho-associated protein kinase 2Homo sapiens (human)
RNA bindingRho-associated protein kinase 2Homo sapiens (human)
protein serine/threonine kinase activityRho-associated protein kinase 2Homo sapiens (human)
structural molecule activityRho-associated protein kinase 2Homo sapiens (human)
protein bindingRho-associated protein kinase 2Homo sapiens (human)
ATP bindingRho-associated protein kinase 2Homo sapiens (human)
small GTPase bindingRho-associated protein kinase 2Homo sapiens (human)
metal ion bindingRho-associated protein kinase 2Homo sapiens (human)
tau protein bindingRho-associated protein kinase 2Homo sapiens (human)
tau-protein kinase activityRho-associated protein kinase 2Homo sapiens (human)
endopeptidase activator activityRho-associated protein kinase 2Homo sapiens (human)
Rho-dependent protein serine/threonine kinase activityRho-associated protein kinase 2Homo sapiens (human)
protein serine kinase activityRho-associated protein kinase 2Homo sapiens (human)
magnesium ion bindingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein kinase activitycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein serine/threonine kinase activitycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
AMP-activated protein kinase activitycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cAMP-dependent protein kinase activitycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein serine/threonine/tyrosine kinase activitycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein bindingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
ATP bindingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein kinase bindingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein domain specific bindingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
manganese ion bindingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
ubiquitin protein ligase bindingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein kinase A regulatory subunit bindingcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
channel activator activitycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein serine kinase activitycAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
protein bindingCyclin-CHomo sapiens (human)
identical protein bindingCyclin-CHomo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-CHomo sapiens (human)
protein kinase activityCyclin-dependent kinase 8Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 8Homo sapiens (human)
protein bindingCyclin-dependent kinase 8Homo sapiens (human)
ATP bindingCyclin-dependent kinase 8Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 8Homo sapiens (human)
ubiquitin protein ligase activityCyclin-dependent kinase 8Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 8Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 8Homo sapiens (human)
protein kinase activityRho-associated protein kinase 1Homo sapiens (human)
protein serine/threonine kinase activityRho-associated protein kinase 1Homo sapiens (human)
protein bindingRho-associated protein kinase 1Homo sapiens (human)
ATP bindingRho-associated protein kinase 1Homo sapiens (human)
small GTPase bindingRho-associated protein kinase 1Homo sapiens (human)
metal ion bindingRho-associated protein kinase 1Homo sapiens (human)
tau protein bindingRho-associated protein kinase 1Homo sapiens (human)
tau-protein kinase activityRho-associated protein kinase 1Homo sapiens (human)
Rho-dependent protein serine/threonine kinase activityRho-associated protein kinase 1Homo sapiens (human)
protein serine kinase activityRho-associated protein kinase 1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 19Homo sapiens (human)
ATP bindingCyclin-dependent kinase 19Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 19Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 19Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (37)

Processvia Protein(s)Taxonomy
nucleusRho-associated protein kinase 2Homo sapiens (human)
centrosomeRho-associated protein kinase 2Homo sapiens (human)
cytosolRho-associated protein kinase 2Homo sapiens (human)
plasma membraneRho-associated protein kinase 2Homo sapiens (human)
cytoplasmic ribonucleoprotein granuleRho-associated protein kinase 2Homo sapiens (human)
centrosomeRho-associated protein kinase 2Homo sapiens (human)
cytoskeletonRho-associated protein kinase 2Homo sapiens (human)
cytoplasmRho-associated protein kinase 2Homo sapiens (human)
axonemecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cytoplasmcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
acrosomal vesiclecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
nucleuscAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
nucleoplasmcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cytoplasmcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
mitochondrial matrixcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
centrosomecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cytosolcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
plasma membranecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
nuclear speckcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
neuromuscular junctioncAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
sperm flagellumcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
dendritic spinecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
plasma membrane raftcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
extracellular exosomecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
ciliary basecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
glutamatergic synapsecAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cAMP-dependent protein kinase complexcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
calcium channel complexcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cytosolcAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
nucleuscAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-CHomo sapiens (human)
nucleoplasmCyclin-CHomo sapiens (human)
CKM complexCyclin-CHomo sapiens (human)
nucleusCyclin-CHomo sapiens (human)
mediator complexCyclin-CHomo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 8Homo sapiens (human)
nucleusCyclin-dependent kinase 8Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 8Homo sapiens (human)
nucleolusCyclin-dependent kinase 8Homo sapiens (human)
CKM complexCyclin-dependent kinase 8Homo sapiens (human)
ubiquitin ligase complexCyclin-dependent kinase 8Homo sapiens (human)
mediator complexCyclin-dependent kinase 8Homo sapiens (human)
protein-containing complexCyclin-dependent kinase 8Homo sapiens (human)
nucleusCyclin-dependent kinase 8Homo sapiens (human)
Golgi membraneRho-associated protein kinase 1Homo sapiens (human)
ruffleRho-associated protein kinase 1Homo sapiens (human)
extracellular regionRho-associated protein kinase 1Homo sapiens (human)
centrioleRho-associated protein kinase 1Homo sapiens (human)
cytosolRho-associated protein kinase 1Homo sapiens (human)
cytoskeletonRho-associated protein kinase 1Homo sapiens (human)
plasma membraneRho-associated protein kinase 1Homo sapiens (human)
cytoplasmic stress granuleRho-associated protein kinase 1Homo sapiens (human)
lamellipodiumRho-associated protein kinase 1Homo sapiens (human)
blebRho-associated protein kinase 1Homo sapiens (human)
secretory granule lumenRho-associated protein kinase 1Homo sapiens (human)
Schaffer collateral - CA1 synapseRho-associated protein kinase 1Homo sapiens (human)
cytoskeletonRho-associated protein kinase 1Homo sapiens (human)
cytoplasmRho-associated protein kinase 1Homo sapiens (human)
cytoplasmic stress granuleRho-associated protein kinase 1Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 19Homo sapiens (human)
cytosolCyclin-dependent kinase 19Homo sapiens (human)
perinuclear region of cytoplasmCyclin-dependent kinase 19Homo sapiens (human)
CKM complexCyclin-dependent kinase 19Homo sapiens (human)
nucleusCyclin-dependent kinase 19Homo sapiens (human)
cytosolCyclin-dependent kinase 19Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID1345316Human Rho associated coiled-coil containing protein kinase 1 (Rho kinase)2009Angewandte Chemie (International ed. in English), , Volume: 48, Issue:47
Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11.
AID1345673Human cyclin dependent kinase 19 (CDK8 subfamily)2009Angewandte Chemie (International ed. in English), , Volume: 48, Issue:47
Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11.
AID1345661Human cyclin dependent kinase 8 (CDK8 subfamily)2009Angewandte Chemie (International ed. in English), , Volume: 48, Issue:47
Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11.
AID1345327Human Rho associated coiled-coil containing protein kinase 2 (Rho kinase)2009Angewandte Chemie (International ed. in English), , Volume: 48, Issue:47
Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11.
AID1613749Binding affinity to wild-type partial length human PKACalpha (G10 to F351 residues) expressed in bacterial expression system by Kinomescan assay2019European journal of medicinal chemistry, Feb-15, Volume: 164CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
AID1613750Antiproliferative activity against VEGF-stimulated HUVEC2019European journal of medicinal chemistry, Feb-15, Volume: 164CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
AID1388660Growth inhibition of human SKNO1 cells after 10 days by CellTiter-Glo assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1613751Cytotoxicity against NHDF cells2019European journal of medicinal chemistry, Feb-15, Volume: 164CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
AID1388657Inhibition of CDK19 (unknown origin) in presence of [gamma33P]ATP by radiometric method2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1474304Inhibition of CDK8 (unknown origin) assessed as reduction in RNAP2 C-terminal domain phosphorylation2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3',4':3,4]benzo[1,2-d]isothiazole derivatives.
AID1474305Antitumor activity against human SET2 cells implanted in AML patients assessed as reduction in tumor volume administered intraperitoneally relative to control2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3',4':3,4]benzo[1,2-d]isothiazole derivatives.
AID1613744Binding affinity to wild-type partial length human CDK8 (M1 to T360 residues) expressed in bacterial expression system by Kinomescan assay2019European journal of medicinal chemistry, Feb-15, Volume: 164CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
AID1388662Growth inhibition of human SET2 cells after 10 days by CellTiter-Glo assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1613747Binding affinity to wild-type partial length human ROCK1 (M1 to R415 residues) expressed in mammalian expression system by Kinomescan assay2019European journal of medicinal chemistry, Feb-15, Volume: 164CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
AID1388661Growth inhibition of human RS4:11 cells after 10 days by CellTiter-Glo assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1388658Inhibition of ROCK1 (unknown origin)2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1388664Growth inhibition of human MV4-11 cells after 10 days by CellTiter-Glo assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1613746Binding affinity to wild-type partial length human CDK11 (M1 to N360 residues) expressed in bacterial expression system by Kinomescan assay2019European journal of medicinal chemistry, Feb-15, Volume: 164CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
AID1388663Growth inhibition of human MOLM14 cells after 10 days by CellTiter-Glo assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1388667Growth inhibition of human TF1 cells after 10 days by CellTiter-Glo assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1388655Antitumor activity against human SET2 cells xenografted in SCID Beige mouse assessed as tumor growth inhibition at 0.16 mg/kg, ip qd measured on day 33 relative to control2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1388668Growth inhibition of human HCT116 cells after 7 days by CellTiter-Glo assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1388659Inhibition of ROCK2 (unknown origin)2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1613748Binding affinity to wild-type partial length human ROCK2 (M1 to T431 residues) expressed in mammalian expression system by Kinomescan assay2019European journal of medicinal chemistry, Feb-15, Volume: 164CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
AID1388665Growth inhibition of human UKE1 cells after 10 days by CellTiter-Glo assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1613752Selectivity index, ratio of IC50 for NHDF cells to IC50 for VEGF-stimulated HUVEC2019European journal of medicinal chemistry, Feb-15, Volume: 164CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
AID1388656Inhibition of CDK8/CCNC (unknown origin) using RBER-IRStide as substrate in presence of [gamma33P]ATP by radiometric method2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1388666Growth inhibition of human MEG01 cells after 10 days by CellTiter-Glo assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (29)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's8 (27.59)29.6817
2010's21 (72.41)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 30.69

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

MetricThis Compound (vs All)
Research Demand Index30.69 (24.57)
Research Supply Index3.40 (2.92)
Research Growth Index4.61 (4.65)
Search Engine Demand Index30.68 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (30.69)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (10.34%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other26 (89.66%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
isoquinoline
[no description available]		2.4620azaarene;
isoquinolines;
mancude organic heterobicyclic parent;
ortho-fused heteroarene
cyclopentane
Cyclopentanes: A group of alicyclic hydrocarbons with the general formula R-C5H9.. cyclopentanes : Cyclopentane and its derivatives formed by substitution.		2.0510cycloalkane;
cyclopentanes;
volatile organic compound		non-polar solvent
gold
Gold: A yellow metallic element with the atomic symbol Au, atomic number 79, and atomic weight 197. It is used in jewelry, goldplating of other metals, as currency, and in dental restoration. Many of its clinical applications, such as ANTIRHEUMATIC AGENTS, are in the form of its salts.		2.0510copper group element atom;
elemental gold
phenyl acetate
phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.		2.0510benzenes;
phenyl acetates
alkenes
[no description available]		2.0510
sorafenib
[no description available]		4.220(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
2-amino-6-methyl-4-(3-pyridinyl)-5,6,7,8-tetrahydroquinoline-3-carbonitrile
[no description available]		4.220bipyridines
vitamin d 2
Ergocalciferols: Derivatives of ERGOSTEROL formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. They differ from CHOLECALCIFEROL in having a double bond between C22 and C23 and a methyl group at C24.. vitamin D2 : A vitamin D supplement and has been isolated from alfalfa.		2.0810hydroxy seco-steroid;
seco-ergostane;
vitamin D		bone density conservation agent;
nutraceutical;
plant metabolite;
rodenticide
cp 724714
2-methoxy-N-(3-(4-((3-methyl-4-((6-methyl-3-pyridinyl)oxy)phenyl)amino)-6-quinazolinyl)-2-propenyl)acetamide: CP-724714 is the ((2E)-isomer, 1:1.5 succinate); structure in first source		3.31102-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamideantineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
hepatotoxic agent
abt 869
[no description available]		3.2710aromatic amine;
indazoles;
phenylureas		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
cortistatin 14
cortistatin: a cortical neuropeptide; shows strong structural similarity to somatostatin; a neuronal depressant; has sleep-modulating activity; amino acid sequence given in first source		2.0610
levobunolol
cortistatin J: structure in first source		2.9840
didehydro-cortistatin a
didehydro-cortistatin A: has anti-HIV activity; structure in first source		2.0710
incb-018424
[no description available]		2.1510nitrile;
pyrazoles;
pyrrolopyrimidine		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
gsk1210151a
GSK1210151A: inhibitor of the BET family of proteins; structure in first source		2.1110imidazoquinoline
CCT251545
CCT251545: a Wnt signaling inhibitor; structure in first source. CCT251545 : A chloropyridine that is 3-chloropyridine substituted by a 1-oxo-2,8-diazaspiro[4.5]decan-8-yl group and a 4-(1-methyl-1H-pyrazol-4-yl)phenyl group at positions 4 and 5, respectively. It is an orally bioavailable inhibitor of Wnt signaling (IC50 = 5 nM) and a potent and selective chemical probe for cyclin-dependent kinases CDK8 and CDK19.		2.1310azaspiro compound;
chloropyridine;
pyrazoles		antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
Wnt signalling inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Benign Neoplasms
[description not available]		03.9820
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		03.9820
Colorectal Cancer
[description not available]		03.1210
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		03.1210
Acute Myelogenous Leukemia
[description not available]		02.8130
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		02.8130
Disease Exacerbation
[description not available]		02.1110
Angiogenesis, Pathologic
[description not available]		02.0610
HIV Coinfection
[description not available]		02.0710
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		02.0710