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Literature summary extracted from

  • Leitch, A.E.; Haslett, C.; Rossi, A.G.
    Cyclin-dependent kinase inhibitor drugs as potential novel anti-inflammatory and pro-resolution agents (2009), Br. J. Pharmacol., 158, 1004-1016.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.22 (R)-roscovitine specific inhibitor of CDK1, 2, 5, and 7 Homo sapiens
2.7.11.22 6-dimethylamino purine potent inhibitor of CDK1/cyclin B Homo sapiens
2.7.11.22 alsterpaullone
-
 Homo sapiens
2.7.11.22 aminopurvalanol
-
 Homo sapiens
2.7.11.22 fascaplysin CDK4- and CDK6-specific inhibitor Homo sapiens
2.7.11.22 flavopiridol non-specific CDK inhibitor Homo sapiens
2.7.11.22 H717
-
 Homo sapiens
2.7.11.22 hymenialdisine
-
 Homo sapiens
2.7.11.22 isopentenyladenine potent inhibitor of CDK1/cyclin B Homo sapiens
2.7.11.22 meriolin
-
 Homo sapiens
2.7.11.22 NU-2058
-
 Homo sapiens
2.7.11.22 NU-6027
-
 Homo sapiens
2.7.11.22 OL567
-
 Homo sapiens
2.7.11.22 Olomoucine specific inhibitor of CDK1, 2, 5, and 7 Homo sapiens
2.7.11.22 olomoucine II
-
 Homo sapiens
2.7.11.22 p21 also named WAF1, SD1,or Cip1, specific inhibitor of CDK2, 4 and 6 Homo sapiens
2.7.11.22 PD183812
-
 Homo sapiens
2.7.11.22 purvalanol B specific inhibitor of CDK1, 2, 5, and 7 Homo sapiens
2.7.11.22 staurosporine potent inhibitor of CDK1/cyclin B Homo sapiens
2.7.11.22 SU-9516
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.22 ATP + CDK1 Homo sapiens CDK7 phosphorylates the activation segment or T-loop of CDK1 ADP + phosphorylated CDK1
-
 ?
2.7.11.22 ATP + cdk2 Homo sapiens CDK7 phosphorylates the activation segment or T-loop of CDK2 ADP + phosphorylated cdk2
-
 ?
2.7.11.22 ATP + RNA polymerase II Homo sapiens CDK7 and CDK8 phosphorylate the C-terminal domain of RNA Pol II ADP + phosphorylated RNA polymerase II
-
 ?
2.7.11.22 ATP + STAT3 Homo sapiens substrate of CDK5 ADP + phosphorylated STAT3
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.22 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.22 granulocyte
-
 Homo sapiens
-
2.7.11.22 lymphocyte
-
 Homo sapiens
-
2.7.11.22 neutrophil
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.22 ATP + CDK1 CDK7 phosphorylates the activation segment or T-loop of CDK1 Homo sapiens ADP + phosphorylated CDK1
-
 ?
2.7.11.22 ATP + cdk2 CDK7 phosphorylates the activation segment or T-loop of CDK2 Homo sapiens ADP + phosphorylated cdk2
-
 ?
2.7.11.22 ATP + RNA polymerase II CDK7 and CDK8 phosphorylate the C-terminal domain of RNA Pol II Homo sapiens ADP + phosphorylated RNA polymerase II
-
 ?
2.7.11.22 ATP + STAT3 substrate of CDK5 Homo sapiens ADP + phosphorylated STAT3
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.22 Cdk1
-
 Homo sapiens
2.7.11.22 CDK10
-
 Homo sapiens
2.7.11.22 CDK11
-
 Homo sapiens
2.7.11.22 CDK2
-
 Homo sapiens
2.7.11.22 CDK3
-
 Homo sapiens
2.7.11.22 CDK4
-
 Homo sapiens
2.7.11.22 Cdk5
-
 Homo sapiens
2.7.11.22 cdk6
-
 Homo sapiens
2.7.11.22 cdk7
-
 Homo sapiens
2.7.11.22 CDK8
-
 Homo sapiens
2.7.11.22 CDK9
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.22 ATP
-
 Homo sapiens
2.7.11.22 cyclin A cofactor of CDK2 Homo sapiens
2.7.11.22 cyclin B cofactor of CDK1 Homo sapiens
2.7.11.22 cyclin C cofactor of CDK3 Homo sapiens
2.7.11.22 cyclin D cofactor of CDK4 and CDK6 Homo sapiens
2.7.11.22 cyclin D3 cofactor of CDK11 Homo sapiens
2.7.11.22 cyclin E cofactor of CDK2 Homo sapiens
2.7.11.22 cyclin E2 cofactor of CDK3 Homo sapiens
2.7.11.22 cyclin H cofactor of CDK7 Homo sapiens
2.7.11.22 cyclin L cofactor of CDK11 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.22 0.000006
-
 CDK1 Homo sapiens staurosporine
2.7.11.22 0.000006
-
 CDK1 Homo sapiens purvalanol B
2.7.11.22 0.000006
-
 CDK5 Homo sapiens purvalanol B
2.7.11.22 0.000006
-
 CDK9 Homo sapiens flavopiridol
2.7.11.22 0.000007
-
 CDK2 Homo sapiens staurosporine
2.7.11.22 0.000008
-
 CDK4 Homo sapiens PD183812
2.7.11.22 0.000009
-
 CDK2 Homo sapiens purvalanol B
2.7.11.22 0.00002
-
 CDK5 Homo sapiens aminopurvalanol
2.7.11.22 0.000022
-
 CDK1 Homo sapiens hymenialdisine
2.7.11.22 0.000026
-
 CDK9 Homo sapiens meriolin
2.7.11.22 0.000028
-
 CDK2 Homo sapiens aminopurvalanol
2.7.11.22 0.000028
-
 CDK5 Homo sapiens hymenialdisine
2.7.11.22 0.000033
-
 CDK1 Homo sapiens aminopurvalanol
2.7.11.22 0.000035
-
 CDK1 Homo sapiens alsterpaullone
2.7.11.22 0.00004
-
 CDK1 Homo sapiens SU-9516
2.7.11.22 0.00004
-
 CDK2 Homo sapiens hymenialdisine
2.7.11.22 0.00004
-
 CDK5 Homo sapiens alsterpaullone
2.7.11.22 0.00005
-
 CDK2 Homo sapiens H717
2.7.11.22 0.00006
-
 CDK1 Homo sapiens flavopiridol
2.7.11.22 0.00006
-
 CDK9 Homo sapiens olomoucine II
2.7.11.22 0.00009
-
 CDK2 Homo sapiens meriolin
2.7.11.22 0.0001
-
 CDK2 Homo sapiens olomoucine II
2.7.11.22 0.00013
-
 CDK2 Homo sapiens (R)-roscovitine
2.7.11.22 0.00015
-
 CDK2 Homo sapiens flavopiridol
2.7.11.22 0.00016
-
 CDK5 Homo sapiens (R)-roscovitine
2.7.11.22 0.00017
-
 CDK2 Homo sapiens PD183812
2.7.11.22 0.00017
-
 CDK5 Homo sapiens flavopiridol
2.7.11.22 0.0002
-
 CDK2 Homo sapiens alsterpaullone
2.7.11.22 0.0002
-
 CDK4 Homo sapiens SU-9516
2.7.11.22 0.00023
-
 CDK1 Homo sapiens H717
2.7.11.22 0.00023
-
 CDK1 Homo sapiens OL567
2.7.11.22 0.0003
-
 CDK7 Homo sapiens flavopiridol
2.7.11.22 0.00035
-
 CDK4 Homo sapiens fascaplysin
2.7.11.22 0.0004
-
 CDK4 Homo sapiens flavopiridol
2.7.11.22 0.00045
-
 CDK1 Homo sapiens (R)-roscovitine
2.7.11.22 0.00045
-
 CDK7 Homo sapiens olomoucine II
2.7.11.22 0.00049
-
 CDK7 Homo sapiens (R)-roscovitine
2.7.11.22 0.00051
-
 CDK5 Homo sapiens meriolin
2.7.11.22 0.0006
-
 CDK4 Homo sapiens hymenialdisine
2.7.11.22 0.00074
-
 CDK9 Homo sapiens (R)-roscovitine
2.7.11.22 0.00078
-
 CDK1 Homo sapiens meriolin
2.7.11.22 0.0013
-
 CDK2 Homo sapiens NU-6027
2.7.11.22 0.0025
-
 CDK1 Homo sapiens NU-6027
2.7.11.22 0.003
-
 CDK5 Homo sapiens Olomoucine
2.7.11.22 0.005
-
 CDK1 Homo sapiens NU-2058
2.7.11.22 0.007
-
 CDK1 Homo sapiens Olomoucine
2.7.11.22 0.007
-
 CDK2 Homo sapiens Olomoucine
2.7.11.22 0.0076
-
 CDK1 Homo sapiens olomoucine II
2.7.11.22 0.01
-
 IC50 above 0.01 mM, CDK4 Homo sapiens staurosporine
2.7.11.22 0.01
-
 IC50 above 0.01 mM, CDK4 Homo sapiens alsterpaullone
2.7.11.22 0.01
-
 IC50 above 0.01 mM, CDK4 Homo sapiens purvalanol B
2.7.11.22 0.012
-
 CDK2 Homo sapiens NU-2058
2.7.11.22 0.0142
-
 CDK4 Homo sapiens (R)-roscovitine
2.7.11.22 0.0198
-
 CDK4 Homo sapiens olomoucine II
2.7.11.22 0.02
-
 CDK5 Homo sapiens fascaplysin
2.7.11.22 0.04
-
 IC50 above 0.04 mM, CDK1 Homo sapiens PD183812
2.7.11.22 0.05
-
 IC50 above 0.05 mM, CDK2 Homo sapiens fascaplysin
2.7.11.22 0.1
-
 IC50 above 0.1 mM, CDK1 Homo sapiens fascaplysin
2.7.11.22 1
-
 IC50 above 1.0 mM, CDK4 Homo sapiens Olomoucine

General Information

EC Number General Information Comment Organism
2.7.11.22 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