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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V55067 | Avotaciclib (BEY1107) | 1983983-41-0 | Avotaciclib (BEY1107) is a potent and orally bioactive cyclin dependent kinase 1 (CDK1) inhibitor. |
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V77223 | Avotaciclib hydrochloride (BEY1107 hydrochloride) | Avotaciclib HCl is the HCl form of the CDK1 inhibitor Avotaciclib. | |
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V53265 | Avotaciclib trihydrochloride (BEY1107 trihydrochloride) | 1983984-01-5 | Avotaciclib (BEY1107) tri HCl is a potent and orally bioactive cyclin dependent kinase 1 (CDK1) inhibitor. |
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V4060 | AZD4573 | 2057509-72-3 | AZD4573 (AZD-4573) is a novel, potent and short acting inhibitor ofserine/threonine CDK9(cyclin-dependent kinase 9, IC50<0.004 μM) with potential anticancer activities. |
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V1555 | AZD5438 | 602306-29-6 | AZD5438 (AZD-5438;AZD 5438) is a novel, potent and selective small molecule inhibitor of cyclin-dependent kinase (CDK) 1, 2 and 9 with potential antineoplastic activity. |
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V4162 | BAY-1251152 | 1610358-59-2 | BAY-1251152, the enanthiomer of BAY-1251152 which is a potent and highly selective PTEF/CDK9 inhibitor. |
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V4715 | BI-1347 | 2163056-91-3 | BI-1347 is a novel, potent and selective CDK8 inhibitor with an IC50 of 1.1 nM. |
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V4590 | BML-259 | 267654-00-2 | BML-259 is a potent cyclin-dependent kinase 5 (Cdk5) inhibitor (antagonist) with IC50s of 64 and 98 nM for Cdk5 and Cdk2, respectively. |
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V1554 | BMS-265246 | 582315-72-8 | BMS-265246 (BMS265246;BMS 265246) is a novel, potent and selective CDK1/2 (Cyclin-dependent kinases) inhibitor with potential antitumor activity. |
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V5209 | Bohemine | 189232-42-6 | Bohemine, structurally similar to Olomoucine and Roscovitine, is a novel, potent, selective, and cell-permeable cyclin-dependent kinase (CDK) with IC50s of 4.6, 83, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. |
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V17001 | BRD6989 | 642008-81-9 | BRD6989 is an analog of the naturally occurng cortistatin A (dCA), acting as a novel, potent and selective CDK8 inhibitor with an IC50 of ~200 nM. |
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V33939 | BS-181 | 1092443-52-1 | BS-181 HCl is a novel, highly selective, and small molecule CDK7 inhibitor with IC50 of 21 NM in a cell-free assay. |
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V1553 | BS-181 HCl | 1397219-81-6 | BS-181 HCl (BS181; BS 181), the hydrochloride salt of BS181, is a novel, highly selective, and small molecule Cyclin-dependent kinase 7 (CDK7) inhibitor with potential antitumor activity. |
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V52316 | BSJ-03-204 | 2349356-09-6 | BSJ-03-204 is a PROTAC linked by Cereblon ligand and CDK ligand. |
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V52315 | BSJ-04-132 | 2349356-39-2 | BSJ-04-132 is a PROTAC linked by Cereblon ligand and CDK ligand. |
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V80116 | CAF-382 | CAF-382 (compound B1) is an SNS-032 analogue and a CDKL5 and pan-CDK inhibitor (antagonist) with weak GSK3α/β affinity (>1.8 μM) and inhibitory activity. | |
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V17707 | CC-671 | 1618658-88-0 | CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor (antagonist) with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively. |
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V55075 | Cdc7-IN-3 | 1402057-87-7 | Cdc7-IN-3 (compound IA) is a potent Cdc7 kinase inhibitor. |
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V55072 | Cdc7-IN-4 | 1402059-21-5 | Cdc7-IN-4 (compound IC) is a potent Cdc7 kinase inhibitor. |
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V53128 | Cdc7-IN-5 | 1402057-86-6 | Cdc7-IN-5 (compound IB) is a potent Cdc7 kinase inhibitor. |
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