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.
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; acts as molecular glue | |
| 6174 | CVT 313 |
| Cdk2 and cdk5 inhibitor | |
| 7223 | Dabrafenib mesylate New |
| Potent and selective B-Raf, CDK16 and NEK9 inhibitor; anticancer; also targets human proteins in the SARS-CoV-2 interactome | |
| 3610 | (R)-DRF053 dihydrochloride |
| Cdk inhibitor; also potent CK1 inhibitor | |
| 3094 | Flavopiridol hydrochloride |
| Cdk inhibitor; potently inhibits cdk2 and cdk9 | |
| 7158 | FMF-04-159-2 New |
| Potent covalent CDK14 and CDK16 inhibitor; also inhibits other TAIRE kinase family members | |
| 7159 | FMF-04-159-R New |
| Potent CDK14 and CDK16 inhibitor; displays reversible inhibition of CDK14 | |
| 1813 | Indirubin-3'-oxime |
| Cdk inhibitor; also inhibits GSK-3β and other protein kinases | |
| 6789 | K 03861 New |
| Potent Cdk2 inhibitor | |
| 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 | |
| 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 | |
| 7050 | Ribociclib |
| Dual cdk4/cdk6 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 |
| 6921 | BSJ-03-123 |
| Selective Cdk6 degrader | |
| 6938 | BSJ-03-204 |
| Selective Cdk4/6 degrader | |
| 6937 | BSJ-04-132 |
| Selective Cdk4 degrader | |
| 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.
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 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 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 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 |
Our Cancer Research Guide highlights over 750 products for cancer research.
Request copyDownload PDF
Our Kinase listing highlights over 400 products for kinase research.
Request copyDownload PDF
Our Neurodegeneration guide highlights over 275 products for neurodegeneration research.
Request copyDownload PDF
Our Cell Cycle & DNA Damage Repair 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.
Request copyDownload PDF