Any feedback?
Literature summary for 2.7.11.22 extracted from
- Cyclin-dependent kinase inhibitor drugs as potential novel anti-inflammatory and pro-resolution agents (2009), Br. J. Pharmacol., 158, 1004-1016.
Inhibitors
| 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/ Products (Substrates)
| 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
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| granulocyte | - |
Homo sapiens | - |
| lymphocyte | - |
Homo sapiens | - |
| neutrophil | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| 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
| 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
| 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 | 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
| 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 |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
