Page last updated: 2024-08-07 23:33:12

Cyclin-dependent kinase 8

A cyclin-dependent kinase 8 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P49336]

Synonyms

EC 2.7.11.22;
EC 2.7.11.23;
Cell division protein kinase 8;
Mediator complex subunit CDK8;
Mediator of RNA polymerase II transcription subunit CDK8;
Protein kinase K35

Research

Bioassay Publications (23)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (8.70)29.6817
2010's13 (56.52)24.3611
2020's8 (34.78)2.80

Compounds (87)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
indirubinHomo sapiens (human)IC502.200011
staurosporineHomo sapiens (human)IC500.010522
birb 796Homo sapiens (human)IC501.000011
cyc 202Homo sapiens (human)IC500.100011
sorafenibHomo sapiens (human)IC502.01651010
tosylphenylalanyl chloromethyl ketoneHomo sapiens (human)IC5012.500020
2-amino-6-methyl-4-(3-pyridinyl)-5,6,7,8-tetrahydroquinoline-3-carbonitrileHomo sapiens (human)IC500.427844
wogoninHomo sapiens (human)IC505.900011
abt 869Homo sapiens (human)IC502.158033
cortistatin aHomo sapiens (human)IC500.008522
bs 194Homo sapiens (human)IC500.090011
dinaciclibHomo sapiens (human)IC500.003920
bs-181Homo sapiens (human)IC504.200011
CCT251545Homo sapiens (human)IC500.016933
CCT251545Homo sapiens (human)Ki0.009011
ly2857785Homo sapiens (human)IC500.016011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
sb 202190Homo sapiens (human)Kd10.000011
imatinibHomo sapiens (human)Kd10.000022
staurosporineHomo sapiens (human)Kd0.510022
gefitinibHomo sapiens (human)Kd10.000022
lestaurtinibHomo sapiens (human)Kd9.000022
vatalanibHomo sapiens (human)Kd7.250022
ruboxistaurinHomo sapiens (human)Kd10.000022
canertinibHomo sapiens (human)Kd10.000022
birb 796Homo sapiens (human)Kd0.220022
cyc 202Homo sapiens (human)Kd10.000011
sb 203580Homo sapiens (human)Kd10.000022
enzastaurinHomo sapiens (human)Kd10.000011
erlotinibHomo sapiens (human)Kd10.000022
lapatinibHomo sapiens (human)Kd10.000022
sorafenibHomo sapiens (human)Kd0.310044
pd 173955Homo sapiens (human)Kd10.000011
s 1033Homo sapiens (human)Kd10.000011
bms 387032Homo sapiens (human)Kd1.200022
tandutinibHomo sapiens (human)Kd10.000033
vx-745Homo sapiens (human)Kd10.000022
dasatinibHomo sapiens (human)Kd10.000022
zd 6474Homo sapiens (human)Kd10.000022
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamideHomo sapiens (human)Kd10.000011
alvocidibHomo sapiens (human)Kd0.120022
bosutinibHomo sapiens (human)Kd10.000011
su 11248Homo sapiens (human)Kd10.000033
jnj-7706621Homo sapiens (human)Kd10.000011
vx680Homo sapiens (human)Kd10.000022
ekb 569Homo sapiens (human)Kd10.000011
axitinibHomo sapiens (human)Kd10.000011
pd 184352Homo sapiens (human)Kd10.000011
bms345541Homo sapiens (human)Kd10.000011
midostaurinHomo sapiens (human)Kd10.000033
2-pyridin-2-yl-4h-1,3-benzothiazin-4-oneHomo sapiens (human)Kd10.000010
ki 20227Homo sapiens (human)Kd10.000011
cp 724714Homo sapiens (human)Kd2.300022
pi103Homo sapiens (human)Kd10.000022
hki 272Homo sapiens (human)Kd10.000011
tofacitinibHomo sapiens (human)Kd10.000022
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)Kd10.000011
cediranibHomo sapiens (human)Kd10.000011
masitinibHomo sapiens (human)Kd10.000011
pazopanibHomo sapiens (human)Kd10.000022
azd 6244Homo sapiens (human)Kd10.000011
su 14813Homo sapiens (human)Kd10.000022
bibw 2992Homo sapiens (human)Kd10.000011
tg100-115Homo sapiens (human)Kd10.000011
pha 665752Homo sapiens (human)Kd10.000011
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-oneHomo sapiens (human)Kd10.000011
brivanibHomo sapiens (human)Kd10.000011
at 7519Homo sapiens (human)Kd10.000011
bi 2536Homo sapiens (human)Kd10.000011
nvp-ast487Homo sapiens (human)Kd0.001422
kw 2449Homo sapiens (human)Kd10.000011
abt 869Homo sapiens (human)Kd0.095022
cortistatin aHomo sapiens (human)Kd0.017011
gw 2580Homo sapiens (human)Kd10.000022
crizotinibHomo sapiens (human)Kd10.000011
chir-265Homo sapiens (human)Kd10.000022
motesanibHomo sapiens (human)Kd10.000022
mln8054Homo sapiens (human)Kd10.000022
GDC-0879Homo sapiens (human)Kd10.000011
gsk 461364Homo sapiens (human)Kd10.000011
azd 1152-hqpaHomo sapiens (human)Kd10.000022
nvp-tae684Homo sapiens (human)Kd10.000011
fedratinibHomo sapiens (human)Kd10.000011
gsk690693Homo sapiens (human)Kd10.000011
gdc 0941Homo sapiens (human)Kd10.000011
plx 4720Homo sapiens (human)Kd1.900011
sgx 523Homo sapiens (human)Kd10.000011
quizartinibHomo sapiens (human)Kd10.000022
incb-018424Homo sapiens (human)Kd10.000011
gsk 1838705aHomo sapiens (human)Kd10.000011
gsk 1363089Homo sapiens (human)Kd0.130011
chir 258Homo sapiens (human)Kd10.000022
nintedanibHomo sapiens (human)Kd10.000011
pp242Homo sapiens (human)Kd6.300011

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
cyc 202Homo sapiens (human)INH24.500011
olomoucine iiHomo sapiens (human)INH11.400011

Enables

This protein enables 8 target(s):

TargetCategoryDefinition
protein kinase activitymolecular functionCatalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640]
cyclin-dependent protein serine/threonine kinase activitymolecular functionCyclin-dependent catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:pr, GOC:rn, PMID:7877684, PMID:9841670]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
ATP bindingmolecular functionBinding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732]
RNA polymerase II CTD heptapeptide repeat kinase activitymolecular functionCatalysis of the reaction: ATP + RNA polymerase II large subunit CTD heptapeptide repeat (consensus YSPTSPS) = ADP + H+ + phosphorylated RNA polymerase II. [EC:2.7.11.23, GOC:mah, PMID:28248323]
ubiquitin protein ligase activitymolecular functionCatalysis of the transfer of ubiquitin to a substrate protein via the reaction X-ubiquitin + S = X + S-ubiquitin, where X is either an E2 or E3 enzyme, the X-ubiquitin linkage is a thioester bond, and the S-ubiquitin linkage is an amide bond: an isopeptide bond between the C-terminal glycine of ubiquitin and the epsilon-amino group of lysine residues in the substrate or, in the linear extension of ubiquitin chains, a peptide bond the between the C-terminal glycine and N-terminal methionine of ubiquitin residues. [GOC:BioGRID, GOC:dph, GOC:mah, GOC:tb, PMID:22863777]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]
protein serine/threonine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925]

Located In

This protein is located in 3 target(s):

TargetCategoryDefinition
nucleuscellular componentA membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]
nucleoplasmcellular componentThat part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653]
nucleoluscellular componentA small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
nucleuscellular componentA membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]

Part Of

This protein is part of 5 target(s):

TargetCategoryDefinition
cyclin-dependent protein kinase holoenzyme complexcellular componentCyclin-dependent protein kinases (CDKs) are enzyme complexes that contain a kinase catalytic subunit associated with a regulatory cyclin partner. [GOC:krc, PMID:11602261]
CKM complexcellular componentCyclin-dependent kinase complex which reversibly associates with the Mediator complex. In Saccharomyces cerevisiae it consists of SSN2, SSN3, SSN8 and SRB8. [GOC:bhm, PMID:12200444]
ubiquitin ligase complexcellular componentA protein complex that includes a ubiquitin-protein ligase and enables ubiquitin protein ligase activity. The complex also contains other proteins that may confer substrate specificity on the complex. [GOC:jh2, PMID:9529603]
mediator complexcellular componentA protein complex that interacts with the carboxy-terminal domain of the largest subunit of RNA polymerase II and plays an active role in transducing the signal from a transcription factor to the transcriptional machinery. The mediator complex is required for activation of transcription of most protein-coding genes, but can also act as a transcriptional corepressor. The Saccharomyces complex contains several identifiable subcomplexes: a head domain comprising Srb2, -4, and -5, Med6, -8, and -11, and Rox3 proteins; a middle domain comprising Med1, -4, and -7, Nut1 and -2, Cse2, Rgr1, Soh1, and Srb7 proteins; a tail consisting of Gal11p, Med2p, Pgd1p, and Sin4p; and a regulatory subcomplex comprising Ssn2, -3, and -8, and Srb8 proteins. Metazoan mediator complexes have similar modular structures and include homologs of yeast Srb and Med proteins. [PMID:11454195, PMID:16168358, PMID:17870225]
protein-containing complexcellular componentA stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah]

Involved In

This protein is involved in 5 target(s):

TargetCategoryDefinition
protein ubiquitinationbiological processThe process in which one or more ubiquitin groups are added to a protein. [GOC:ai]
positive regulation of transcription by RNA polymerase IIbiological processAny process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH]
regulation of cell cyclebiological processAny process that modulates the rate or extent of progression through the cell cycle. [GOC:ai, GOC:dph, GOC:tb]
negative regulation of triglyceride metabolic processbiological processAny process that decreases the frequency, rate or extent of the chemical reactions and pathways involving triglyceride, any triester of glycerol. [GOC:dph, GOC:sl, GOC:tb]
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]