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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V85475 | JA397 | ||
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V53248 | JH-XVI-178 | 2648453-53-4 | JH-XVI-178 is a potent and specific CDK8/19 inhibitor (antagonist) with low clearance and moderate oral pharmacokinetic properties. |
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V22999 | JSH-150 | 2247481-21-4 | JSH-150 is a potent and specific CDK9 inhibitor (antagonist) with IC50 of 1 nM. |
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V51912 | K00546 | 443798-47-8 | K00546 is a potent CDK1 and CDK2 inhibitor (antagonist) with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. |
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V1536 | K03861 (AUZ 454) | 853299-07-7 | K03861 (K0 3861;AUZ-454;K-03861;AUZ 454), an aminopyrimidine-phenyl urea analog, is novel and potent type IIcyclin-dependent kinase-CDK2 inhibitor with potential anticancer activity. |
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V51906 | KB-0742 dihydrochloride | 2416874-75-2 | KB-0742 di-HCl is a specific and orally bioactive CDK9 inhibitor (antagonist) with IC50 of 6 nM against CDK9/cyclin T1. |
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V3640 | Kenpaullone | 142273-20-9 | Kenpaullone (NSC-664704) is a novel, potent and ATP competitive inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. |
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V51903 | KH-CB20 | 1354448-60-4 | KH-CB20, an E/Z mixture, is a potent and specific inhibitor of CLK1 and the closely related isoform CLK4, with IC50 for CLK1 inhibition of 16.5 nM. |
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V84703 | KuWal151 | 2341841-06-1 | |
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V1544 | LDC000067 (LDC067) | 1073485-20-7 | LDC000067 (also called LDC-000067;LDC-067) is a novel, potent, highly selective and ATP-competitive inhibitor ofcyclin-dependent kinase (CDK9)with potential antineoplastic activity. |
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V2731 | LDC4297 | 1453834-21-3 | LDC4297 is a novel and potentCDK7 (Cyclin-dependent protein kinase 7) inhibitor with IC50 of 0.13±0.06 nM for CDK7and IC50s between 10 nM and 10,000 nM for all other analyzed CDKs. |
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V51877 | LDC4297 hydrochloride | 2319747-14-1 | LDC4297 HCl is a selective inhibitor of CDK7 with IC50 of 0.13 nM. |
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V5216 | Lerociclib (G1T38) | 1628256-23-4 | Lerociclib (G1T38) is a novel, potent, orally bioavailable and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively. |
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V14767 | Leucettine L41 | 1112978-84-3 | Leucettine L41 is a novel and potent dual inhibitor of both cdc2-like kinase (CLKs) and DYRKs. |
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V51869 | Leucettinib-92 | 2732859-57-1 | Leucettinib-92 (compound 92) is an inhibitor (blocker/antagonist) of DYRK/CLK kinase, with IC50s of 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3). |
CC(C4)C3)C(%3dO)CN5C%3dC(C%3dN5)C6%3dCC%3dC(C%3dC6)C7%3dCN%3dCC8%3dCC%3dCC%3dC87)
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V51029 | LL-K8-22 | LL-K8-22 is a novel CDK8-cyclin C dual degrader that has DC50 values of 2.52 and 2.64 μM, in that order. | |
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V84720 | LL-K9-3 | 2809353-52-2 | |
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V4870 | LY3177833 | 1627696-51-8 | LY3177833, a novel and potent CDC7 (Cell Division Cycle 7-related Protein Kinase) and pMCM2 inhibitor with IC50 values of 3.3 nM and 290 nM, respectively, was extracted from patent US 20140275131 and patent WO 2014143601 A1 compound 4. |
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V51830 | M2N12 | 2376577-06-7 | M2N12 is a potent and selective inhibitor of cell division cycle protein phosphatase 25C (Cdc25C) with IC50 of 0.09 μM. |
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V1551 | Manidipine 2HCl | 89226-75-5 | Manidipine 2HCl (alsocalled CV-4093;CV4093), the dihydrochloride saltform of Manidipine, is a calcium channel blocker/CCB that is used clinically as an antihypertensive agent. |
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