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
6400 Alsterpaullone
Potent cdk1 and cdk2 inhibitor; also inhibits GSK-3β and Lck
2072 Aminopurvalanol A
Selective cdk inhibitor; potently inhibits cdk1, cdk2 and cdk5
2457 Arcyriaflavin A
Potent cdk4 inhibitor; also potently inhibits CaM kinase II; antiviral
3968 AZD 5438
Cdk inhibitor; potently inhibits cdk1, 2, 5 and 9
3194 BIO
Cdk inhibitor; also potent GSK-3 inhibitor
5654 BMS 265246
Cdk inhibitor; potently inhibits cdk1 and cdk2
6438 BRD 6989
Cdk8 inhibitor; enhances IL-10 production
5608 BS 181 dihydrochloride
Selective cdk7 inhibitor
5471 CGP 60474
Potent cdk inhibitor
5472 CGP 74514 dihydrochloride
Potent cdk1 inhibitor
3605 (R)-CR8
Cdk inhibitor; potently inhibits cdk1 and cdk2; also inhibits CK1
6174 CVT 313
Cdk2 and cdk5 inhibitor
3610 (R)-DRF053 dihydrochloride
Cdk inhibitor; also potent CK1 inhibitor
3094 Flavopiridol hydrochloride
Cdk inhibitor; potently inhibits cdk2 and cdk9
1813 Indirubin-3'-oxime
Cdk inhibitor; also inhibits GSK-3β and other protein kinases
1398 Kenpaullone
Cdk inhibitor; also inhibits GSK-3β
6752 LDC 000067
Potent and selective CDK9 inhibitor
2152 NSC 625987
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
Cdk2 inhibitor; also potent inhibitor of aurora kinase A and B
6535 NVP 2
Potent and selective ATP-competitive CDK9 inhibitor
1284 Olomoucine
Cdk inhibitor
1902 [Ala92]-p16 (84-103)
Cdk inhibitor
4786 PD 0332991 isethionate
Potent cdk4 and cdk6 inhibitor; brain penetrant
3140 PHA 767491 hydrochloride
Cdk inhibitor; potently inhibits cdk9; also inhibits MK2
1580 Purvalanol A
Cdk inhibitor; potently inhibits cdk1, cdk2 and cdk5
1581 Purvalanol B
Selective cdk inhibitor; potently inhibits cdk1, cdk2 and cdk5
5494 R 547
Potent and selective cdk inhibitor; orally bioavailable
4181 Ro 3306
Cdk1 inhibitor
1332 Roscovitine
Cdk inhibitor
2609 Ryuvidine
Cdk4 inhibitor; also SETD8 inhibitor
4875 Senexin A
Cdk8 inhibitor
4075 SNS 032
Cdk inhibitor; potently inhibits cdk2, cdk7 and cdk9
2907 SU 9516
Cdk inhibitor; potently inhibits cdk1 and cdk2

Other

Cat No Product Name / Activity
6532 THAL SNS 032
Potent and selective cdk9 degrading PROTAC

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.

External sources of pharmacological information for Cyclin-Dependent Protein Kinases :

    Literature for Cyclin-Dependent Protein Kinases

    Tocris offers the following scientific literature for Cyclin-Dependent Protein Kinases to showcase our products. We invite you to request* or download your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.


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    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