CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle.Additionally, they control mRNA processing, transcription, and nerve cell differentiation. With molecular weights between 34 and 40 kDa, CDKs are relatively small proteins that only contain the kinase domain. In fact, when their CDK gene has been replaced with the homologous human gene, yeast cells can proliferate normally. A CDK by definition binds the control protein cyclin. Only the cyclin-CDK complex is an active kinase; CDK lacks much kinase activity on its own.
Around 20 Cyclin-dependent kinases (CDK1-20) have been identified as of yet. While CDK 7, 8, 9 and 11 are linked to transcription, CDK1, 4, and 5 are involved in the cell cycle.
The majority of CDK regulation occurs post-translationally, and CDK levels are essentially constant throughout the cell cycle. The majority of knowledge about CDK structure and function is based on CDKs from vertebrates (CDC2 and CDK2), S. pombe (CDC28), and S. cerevisiae (Cdc2). Cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and CDK inhibitory subunit (CKI) binding are the four main mechanisms of CDK regulation.
Structure | Cat No. | Product Name | CAS No. | Product Description |
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V53079 | RSS0680 | 2769753-48-0 | RSS0680 (Example 22) is a bifunctional compound targeting protein-degrading kinases. |
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V5212 | Samuraciclib HCl (ICEC0942; PPDA-001; CT7001) | 1805789-54-1 | Samuraciclib HCl (ICEC-0942; PPDA001; CT-7001), the hydrochloride salt of Samuraciclib, is a novel, potent, orally bioavailable and selective CDK7 inhibitor with potential anticancer activity. |
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V79248 | SB-1295 | SB-1295 is an orally bioactive CDK9/T1 inhibitor (IC50=0.17 μM). | |
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V4557 | SEL120-34A HCl | 1609452-30-3 | SEL120-34A hydrochloride (SEL-120-34A; SEL12034A) is a novel, potent and selective ATP-competitiveinhibitor of CDK8(Cyclin-dependent kinase 8) with anticancer activity. |
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V37095 | SEL120-34A monohydrochloride | 2443816-41-7 | SEL120-34A mono HCl is a selective, ATP-competitive CDK8 inhibitor (antagonist) with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC complexes, respectively, and a Kd of 3 nM for CDK8. |
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V1532 | Seliciclib (Roscovitine) | 186692-46-6 | Seliciclib (also known as Roscovitine, CYC 202; CYC-202;CYC202) is a novel, potent, selective and orally bioavailable small-molecule CDK inhibitor with potential anticancer activity. |
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V2743 | Senexin A | 1366002-50-7 | Senexin A is a novel, potent, selective and ATP site competitive inhibitor of CDK8 and CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19, respectively. |
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V84561 | Senexin A hydrochloride | 1780390-76-2 | |
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V79442 | SHR5428 | SHR5428 is an orally bioavailable, selective non-covalent CDK7 inhibitor (antagonist) with potent CDK7 enzymatic activity (IC50=2.3 nM). | |
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V4595 | Simurosertib | 1330782-76-7 | Simurosertib (formerly known as TAK-931) is a novel, selective and orally bioavailable cycle 7(CDC7, cell division cycle 7-related protein)kinase inhibitor with anticancer activity. |
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V1533 | SNS-032 (BMS-387032) | 345627-80-7 | SNS-032 (also known as BMS-387032; SNS 032; BMS387032; SNS032), a 2-aminothiazole based small-molecule, is a potent and selective inhibitor of CDK2 (cyclin dependent kinase 2) with potential antitumor activity. |
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V2186 | SR-4835 | 2387704-62-1 | SR-4835 (SR4835) is a novel highly selective dual inhibitor of CDK12 and CDK13 with anticancer activity. |
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V1542 | SU9516 | 377090-84-1 | SU 9516 (SU-9516; SU9516), a 3-substituted indolinone, is a potent and selectiveCyclin-dependent kinases (CDKs) inhibitor with potential antineoplastic activity. |
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V55102 | Tacaciclib | 2768774-66-7 | Tacaciclib is a CDK inhibitor (antagonist) with anti-tumor effects. |
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V41738 | Tagtociclib (PF-04457845) | 2460249-19-6 | PF-07104091 (PF07104091) is a novel and orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2) with potential anticancer activity. |
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V53286 | Tanuxiciclib | 1983983-64-7 | Tanuxiciclib is a cyclin-dependent kinase (CDK) inhibitor. |
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V55079 | Tanuxiciclib trihydrochloride | 1983984-11-7 | Tanuxiciclib triHCl is a cyclin-dependent kinase (CDK) inhibitor. |
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V1548 | TG003 | 719277-26-6 | TG003 (TG-003; TG 003) is a novel, potent, selective and ATP-competitive Cdc2-like kinase (Clk) inhibitor with potential anticancer activity. |
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V76416 | THZ1 Hydrochloride | THZ1 HCl is a potent and specific covalent CDK7 inhibitor (antagonist) with IC50 of 3.2 nM. |