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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V77912 | CDK2/Bcl2-IN-1 | CDK2/Bcl2-IN-1 (compound 1) is a saponin and a CDK-2 inhibitor (IC50=117.6 nM) with good cytotoxic effect against cancer cells. | |
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V52282 | Cdk2/Cyclin Inhibitory Peptide I | 237392-84-6 | Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG) is a CDK2 inhibitor that kills U2OS osteosarcoma cells in a dose-dependent fashion. |
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V52281 | Cdk2/Cyclin Inhibitory Peptide II | 237392-85-7 | Cdk2/Cyclin Inhibitory Peptide II (Tat-LDL) is a CDK2 inhibitor that kills U2OS osteosarcoma cells in a dose-dependent fashion. |
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V55080 | CDK4-IN-2 | 2380320-68-1 | CDK4-IN-2 (A17) is an inhibitor (blocker/antagonist) of CDK4 with both Ki and IC50s less than 10 nM. |
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V75979 | CDK4/6-IN-13 | 1908454-70-5 | As a CDK4/6 inhibitor. |
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V52280 | CDK4/6-IN-14 | 2699091-15-9 | CDK4/6-IN-14 is a potent and selective inhibitor of CDK4 and CDK6 (CDK) with IC50 of 10 nM and 16 nM, respectively. |
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V52279 | CDK4/6-IN-15 | 2078047-99-9 | CDK4/6-IN-15 is an orally bioactive and selective CDK4/6 inhibitor. |
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V55088 | CDK4/6-IN-16 | 1169694-98-7 | CDK4/6-IN-16 (example 195) is a potent inhibitor of CDK4 and CDK6 with IC50 of 0.013 μM for CDK4. |
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V55095 | CDK4/6-IN-17 | 2035069-96-4 | CDK4/6-IN-17 (compound 12) is an orally bioactive CDK4/6 inhibitor (antagonist) with IC50 range 10-100 nM in BE(2) cells. |
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V52278 | CDK4/6-IN-3 | 2366237-37-6 | CDK4/6-IN-3 is a brain-penetrating CDK4/CDK6 inhibitor (antagonist) with Ki of <0.3 nM and 2.2 nM respectively. |
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V41999 | CDK4/6-IN-4 | 2138499-06-4 | Abemaciclib metabolite M20 (LSN3106726) is the bioactive metabolite of Abemaciclib and a selective CDK4/6 inhibitor that may be utilized in cancer-related research. |
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V52277 | CDK4/6-IN-5 | 2380321-50-4 | CDK4/6-IN-5 is a potent CDK4 and CDK6 inhibitor (antagonist) with Kis of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3. |
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V55093 | CDK5-IN-1 | 2639540-19-3 | CDK5-IN-1 is a potent CDK5 inhibitor (antagonist) with less than 10 nM activity against CDK5. |
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V55101 | CDK7-IN-10 | 2588110-62-5 | CDK7-IN-10 is a CDK7 inhibitor (antagonist) with IC50 of less than 100 nM, found in patent WO2021016388A1, compound I-1. |
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V52275 | CDK7-IN-11 | 2414896-32-3 | CDK7-IN-11 is an orally bioactive CDK7 inhibitor. |
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V55073 | CDK7-IN-2 hydrochloride hydrate | 2326428-24-2 | CDK7-IN-2 HCl hydrate (Example 6) is a potent and specific CDK7 inhibitor. |
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V55092 | CDK7-IN-21 | 2766124-39-2 | CDK7-IN-21 (compound A22) is a potent CDK7 inhibitor. |
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V55094 | CDK7-IN-22 | 2173190-60-6 | CDK7-IN-22 (compound 101) is a CDK7 inhibitor (antagonist) with anti-tumor activity. |
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V55089 | CDK7-IN-25 | 2009209-60-1 | CDK7-IN-25 (CY-16-1) is a CDK-7 inhibitor (IC50<1nM) and may be utilized in cancer-related research. |
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V78702 | CDK7-IN-26 | CDK7-IN-26 (compound 36) is an orally bioactive CDK7 inhibitor (IC50= 7.4 nM). |
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