Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(R)-roscovitine | specific inhibitor of CDK1, 2, 5, and 7 | Homo sapiens | |
6-dimethylamino purine | potent inhibitor of CDK1/cyclin B | Homo sapiens | |
alsterpaullone | - |
Homo sapiens | |
aminopurvalanol | - |
Homo sapiens | |
fascaplysin | CDK4- and CDK6-specific inhibitor | Homo sapiens | |
flavopiridol | non-specific CDK inhibitor | Homo sapiens | |
H717 | - |
Homo sapiens | |
hymenialdisine | - |
Homo sapiens | |
isopentenyladenine | potent inhibitor of CDK1/cyclin B | Homo sapiens | |
meriolin | - |
Homo sapiens | |
NU-2058 | - |
Homo sapiens | |
NU-6027 | - |
Homo sapiens | |
OL567 | - |
Homo sapiens | |
Olomoucine | specific inhibitor of CDK1, 2, 5, and 7 | Homo sapiens | |
olomoucine II | - |
Homo sapiens | |
p21 | also named WAF1, SD1,or Cip1, specific inhibitor of CDK2, 4 and 6 | Homo sapiens | |
PD183812 | - |
Homo sapiens | |
purvalanol B | specific inhibitor of CDK1, 2, 5, and 7 | Homo sapiens | |
staurosporine | potent inhibitor of CDK1/cyclin B | Homo sapiens | |
SU-9516 | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + CDK1 | Homo sapiens | CDK7 phosphorylates the activation segment or T-loop of CDK1 | ADP + phosphorylated CDK1 | - |
? | |
ATP + cdk2 | Homo sapiens | CDK7 phosphorylates the activation segment or T-loop of CDK2 | ADP + phosphorylated cdk2 | - |
? | |
ATP + RNA polymerase II | Homo sapiens | CDK7 and CDK8 phosphorylate the C-terminal domain of RNA Pol II | ADP + phosphorylated RNA polymerase II | - |
? | |
ATP + STAT3 | Homo sapiens | substrate of CDK5 | ADP + phosphorylated STAT3 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
granulocyte | - |
Homo sapiens | - |
lymphocyte | - |
Homo sapiens | - |
neutrophil | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + CDK1 | CDK7 phosphorylates the activation segment or T-loop of CDK1 | Homo sapiens | ADP + phosphorylated CDK1 | - |
? | |
ATP + cdk2 | CDK7 phosphorylates the activation segment or T-loop of CDK2 | Homo sapiens | ADP + phosphorylated cdk2 | - |
? | |
ATP + RNA polymerase II | CDK7 and CDK8 phosphorylate the C-terminal domain of RNA Pol II | Homo sapiens | ADP + phosphorylated RNA polymerase II | - |
? | |
ATP + STAT3 | substrate of CDK5 | Homo sapiens | ADP + phosphorylated STAT3 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Cdk1 | - |
Homo sapiens |
CDK10 | - |
Homo sapiens |
CDK11 | - |
Homo sapiens |
CDK2 | - |
Homo sapiens |
CDK3 | - |
Homo sapiens |
CDK4 | - |
Homo sapiens |
Cdk5 | - |
Homo sapiens |
cdk6 | - |
Homo sapiens |
cdk7 | - |
Homo sapiens |
CDK8 | - |
Homo sapiens |
CDK9 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens | |
cyclin A | cofactor of CDK2 | Homo sapiens | |
cyclin B | cofactor of CDK1 | Homo sapiens | |
cyclin C | cofactor of CDK3 | Homo sapiens | |
cyclin D | cofactor of CDK4 and CDK6 | Homo sapiens | |
cyclin D3 | cofactor of CDK11 | Homo sapiens | |
cyclin E | cofactor of CDK2 | Homo sapiens | |
cyclin E2 | cofactor of CDK3 | Homo sapiens | |
cyclin H | cofactor of CDK7 | Homo sapiens | |
cyclin L | cofactor of CDK11 | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000006 | - |
CDK1 | Homo sapiens | staurosporine | |
0.000006 | - |
CDK1 | Homo sapiens | purvalanol B | |
0.000006 | - |
CDK5 | Homo sapiens | purvalanol B | |
0.000006 | - |
CDK9 | Homo sapiens | flavopiridol | |
0.000007 | - |
CDK2 | Homo sapiens | staurosporine | |
0.000008 | - |
CDK4 | Homo sapiens | PD183812 | |
0.000009 | - |
CDK2 | Homo sapiens | purvalanol B | |
0.00002 | - |
CDK5 | Homo sapiens | aminopurvalanol | |
0.000022 | - |
CDK1 | Homo sapiens | hymenialdisine | |
0.000026 | - |
CDK9 | Homo sapiens | meriolin | |
0.000028 | - |
CDK2 | Homo sapiens | aminopurvalanol | |
0.000028 | - |
CDK5 | Homo sapiens | hymenialdisine | |
0.000033 | - |
CDK1 | Homo sapiens | aminopurvalanol | |
0.000035 | - |
CDK1 | Homo sapiens | alsterpaullone | |
0.00004 | - |
CDK1 | Homo sapiens | SU-9516 | |
0.00004 | - |
CDK2 | Homo sapiens | hymenialdisine | |
0.00004 | - |
CDK5 | Homo sapiens | alsterpaullone | |
0.00005 | - |
CDK2 | Homo sapiens | H717 | |
0.00006 | - |
CDK1 | Homo sapiens | flavopiridol | |
0.00006 | - |
CDK9 | Homo sapiens | olomoucine II | |
0.00009 | - |
CDK2 | Homo sapiens | meriolin | |
0.0001 | - |
CDK2 | Homo sapiens | olomoucine II | |
0.00013 | - |
CDK2 | Homo sapiens | (R)-roscovitine | |
0.00015 | - |
CDK2 | Homo sapiens | flavopiridol | |
0.00016 | - |
CDK5 | Homo sapiens | (R)-roscovitine | |
0.00017 | - |
CDK2 | Homo sapiens | PD183812 | |
0.00017 | - |
CDK5 | Homo sapiens | flavopiridol | |
0.0002 | - |
CDK2 | Homo sapiens | alsterpaullone | |
0.0002 | - |
CDK4 | Homo sapiens | SU-9516 | |
0.00023 | - |
CDK1 | Homo sapiens | H717 | |
0.00023 | - |
CDK1 | Homo sapiens | OL567 | |
0.0003 | - |
CDK7 | Homo sapiens | flavopiridol | |
0.00035 | - |
CDK4 | Homo sapiens | fascaplysin | |
0.0004 | - |
CDK4 | Homo sapiens | flavopiridol | |
0.00045 | - |
CDK1 | Homo sapiens | (R)-roscovitine | |
0.00045 | - |
CDK7 | Homo sapiens | olomoucine II | |
0.00049 | - |
CDK7 | Homo sapiens | (R)-roscovitine | |
0.00051 | - |
CDK5 | Homo sapiens | meriolin | |
0.0006 | - |
CDK4 | Homo sapiens | hymenialdisine | |
0.00074 | - |
CDK9 | Homo sapiens | (R)-roscovitine | |
0.00078 | - |
CDK1 | Homo sapiens | meriolin | |
0.0013 | - |
CDK2 | Homo sapiens | NU-6027 | |
0.0025 | - |
CDK1 | Homo sapiens | NU-6027 | |
0.003 | - |
CDK5 | Homo sapiens | Olomoucine | |
0.005 | - |
CDK1 | Homo sapiens | NU-2058 | |
0.007 | - |
CDK1 | Homo sapiens | Olomoucine | |
0.007 | - |
CDK2 | Homo sapiens | Olomoucine | |
0.0076 | - |
CDK1 | Homo sapiens | olomoucine II | |
0.01 | - |
IC50 above 0.01 mM, CDK4 | Homo sapiens | staurosporine | |
0.01 | - |
IC50 above 0.01 mM, CDK4 | Homo sapiens | alsterpaullone | |
0.01 | - |
IC50 above 0.01 mM, CDK4 | Homo sapiens | purvalanol B | |
0.012 | - |
CDK2 | Homo sapiens | NU-2058 | |
0.0142 | - |
CDK4 | Homo sapiens | (R)-roscovitine | |
0.0198 | - |
CDK4 | Homo sapiens | olomoucine II | |
0.02 | - |
CDK5 | Homo sapiens | fascaplysin | |
0.04 | - |
IC50 above 0.04 mM, CDK1 | Homo sapiens | PD183812 | |
0.05 | - |
IC50 above 0.05 mM, CDK2 | Homo sapiens | fascaplysin | |
0.1 | - |
IC50 above 0.1 mM, CDK1 | Homo sapiens | fascaplysin | |
1 | - |
IC50 above 1.0 mM, CDK4 | Homo sapiens | Olomoucine |
General Information | Comment | Organism |
---|---|---|
physiological function | CDK1 and CDK2 have integral roles in the cell cycle, putative roles in transcriptional regulation and a controversial role in apoptosis. CDK5 is involved in apoptosis, transcription, differentiation, and endocytosis. CDK7 is a CDK-activating kinase responsible for enhancing the kinase activity of CDK1 and 2. CDK7 associated with cyclin H and MAT1 is responsible for initiation of transcription by the holoenzyme RNA Pol II. Regulation of transcription of Mcl-1 and involvement in pivotal inflammatory signalling via NF-kappaB are functions of CDK7 and CDK9. CDK4 and CDK6 are required for progression through G1 phase. CDK3 is implicated in G0 exit and G1/S phase transition in the cell cycle, CDK10 has a role in transition from G2 to M phase. CDK11 has potentially dual roles in transcription that do not involve direct phosphorylation of RNA polymerase II C-terminal domain. | Homo sapiens |