Cyclin-Dependent Protein Kinases

Cdks (cyclin-dependent kinases) are heteromeric serine/threonine kinases that control progression through the cell cycle in concert with their regulatory subunits, the cyclins. Although there are 12 different cdk genes, only 5 have been shown to directly drive the cell cycle.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
2072 Aminopurvalanol A
Cyclin-dependent kinase inhibitor
2457 Arcyriaflavin A
Potent cdk4/cyclin D1 and CaM Kinase II inhibitor. Antiviral agent (anti-HCMV)
3968 AZD 5438
Potent cyclin-dependent kinase (cdk) 1, 2 and 9 inhibitor
5654 BMS 265246
Potent cdk1/2 inhibitor
5608 BS 181 dihydrochloride
Selective cdk7 inhibitor
5471 CGP 60474
Potent dual cdk1/cdk2 inhibitor
5472 CGP 74514 dihydrochloride
Potent cdk1 inhibitor
3605 (R)-CR8
Dual cdk1/cdk5 inhibitor; also inhibits CK1
6174 CVT 313
cdk2 inhibitor
3610 (R)-DRF053 dihydrochloride
Dual cdk1/cdk5 inhibitor. Also inhibits CK1
3094 Flavopiridol hydrochloride
Cyclin-dependent kinase inhibitor
1532 10Z-Hymenialdisine
Pan kinase inhibitor; potently inhibits Cdk1, Cdk2, Cdk3 and Cdk5
1813 Indirubin-3'-oxime
Cyclin-dependent kinase inhibitor. Also inhibits other protein kinases
1398 Kenpaullone
Potent cyclin-dependent kinase inhibitor. Also inhibits GSK-3
2152 NSC 625987
Cyclin-dependent kinase 4 (cdk4) inhibitor
1867 NSC 663284
Cdc25 phosphatase inhibitor; blocks cdk1 and cdk2 activation
1937 NSC 693868
Cdk inhibitor. Also inhibits GSK-3
3135 NU 2058
Cdk1 and cdk2 inhibitor
3301 NU 6140
Cyclin-dependent kinase 2 (cdk2) inhibitor
1284 Olomoucine
Cyclin-dependent kinase inhibitor
1902 [Ala92]-p16 (84-103)
Cyclin-dependent kinase inhibitor
4786 PD 0332991 isethionate
Potent, selective Cdk4/6 inhibitor; brain penetrant
3140 PHA 767491 hydrochloride
Dual cdc7/cdk9 inhibitor. Also inhibits MK2
1580 Purvalanol A
Cyclin-dependent kinase inhibitor
1581 Purvalanol B
Cyclin-dependent kinase inhibitor
4181 Ro 3306
Cyclin-dependent kinase (cdk) 1 inhibitor
1332 Roscovitine
Potent, selective cyclin-dependent kinase inhibitor
2609 Ryuvidine
Cyclin-dependent kinase 4 (CDK4) inhibitor; also SETD8 inhibitor
4875 Senexin A
Cyclin-dependent kinase 8 (cdk8) inhibitor
4075 SNS 032
Potent cdk2, cdk7 and cdk9 inhibitor
2907 SU 9516
Potent cdk2 inhibitor

Cdks (cyclin-dependent kinases) are heteromeric serine/threonine kinases that control progression through the cell cycle in concert with their regulatory subunits, the cyclins. Although there are 12 different cdk genes, only 5 have been shown to directly drive the cell cycle (Cdk1, -2, -3, -4, and -6).

Following extracellular mitogenic stimuli, cyclin D gene expression is upregulated. Cdk4 forms a complex with cyclin D and phosphorylates Rb protein, leading to liberation of the transcription factor E2F. E2F induces transcription of genes including cyclins A and E, DNA polymerase and thymidine kinase. Cdk4-cyclin E complexes form and initiate G1/S transition. Subsequently, Cdk1-cyclin B complexes form and induce G2/M phase transition. Cdk1-cyclin B activation induces the breakdown of the nuclear envelope and the initiation of mitosis.

Cdks are constitutively expressed and are regulated by several kinases and phosphastases, including Wee1, CDK-activating kinase and Cdc25 phosphatase. In addition, cyclin expression is induced by molecular signals at specific points of the cell cycle, leading to activation of Cdks. Tight control of Cdks is essential as misregulation can induce unscheduled proliferation, and genomic and chromosomal instability. Cdk4 has been shown to be mutated in some types of cancer, whilst a chromosomal rearrangement can lead to Cdk6 overexpression in lymphoma, leukemia and melanoma. Cdks are currently under investigation as potential targets for antineoplastic therapy, but as Cdks are essential for driving each cell cycle phase, therapeutic strategies that block Cdk activity are unlikely to selectively target tumor cells.

Literature for Cyclin-Dependent Protein Kinases

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

  • Alzheimer's disease
  • Parkinson's disease
  • Huntington's disease
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Cyclin-Dependent Kinase (Cdk) Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
Cdk1 Human CDC2 NM_001786 P06493
Mouse Cdc2a NM_007659 P11440
Rat Cdc2a NM_019296 P39951
Cdk2 Human CDK2 NM_001798 P24941
Mouse Cdk2 NM_183417 P97377
Rat Cdk2 NM_199501 Q63699
Cdk3 Human CDK3 NM_001258 Q00526
Mouse Cdk3 NR_004853 Q80YP0
Cdk4 Human CDK4 NM_000075 P11802
Mouse Cdk4 NM_009870 P30285
Rat Cdk4 NM_053593 P35426
Cdk5 Human CDK5 NM_004935 Q00535
Mouse Cdk5 NM_007668 P49615
Rat Cdk5 NM_080885 Q03114
Cdk6 Human CDK6 NM_001259 Q00534
Mouse Cdk6 NM_009873 Q64261
Cdk7 Human CDK7 NM_001799 P50613
Mouse Cdk7 NM_009874 Q03147
Rat Cdk7 X83579 P51952
Cdk8 Human CDK8 NM_001260 P49336
Mouse Cdk8 NM_153599 Q8R3L8
Cdk9 Human CDK9 NM_001261 P50750
Mouse Cdk9 NM_130860 Q99J95
Rat Cdk9 NM_001007743 Q641Z4
Cdk10 Human CDK10 NM_052987 Q15131
Mouse Cdk10 NM_194446 Q3UMM4
Rat Cdk10 NM_001025722 Q4KM47