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 |
|---|---|---|---|---|
|
V55074 | Cdc7-IN-7 | 1402059-17-9 | Cdc7-IN-7 (compound IE) is a potent Cdc7 kinase inhibitor. |
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V55084 | CDK-IN-12 | 2789680-97-1 | CDK-IN-12 (Example 20) is a CDK inhibitor. |
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V35035 | CDK-IN-6 | 779353-02-5 | CDK-IN-6, a class of pyrazolo[1,5-a]pyrimidine compounds, is a CDK inhibitor (antagonist) with anti-cancer effect. |
|
V55100 | CDK/HDAC-IN-1 | 2762181-73-5 | CDK/HDAC-IN-1 showed significant inhibitory effect against CDK2/4/6 and HDAC6 (IC50 = 60.9 ± 2.9, 276 ± 22.3, 27.2 ± 4.2, and 128.6 ± 0.4 nM). |
|
V52284 | CDK1-IN-2 | 220749-41-7 | CDK1-IN-2 is a CDK1 inhibitor (IC50= 5.8 μM). |
|
V52287 | CDK12-IN-4 | 2651196-69-7 | CDK12-IN-4 is a pyrazotriazine and a potent CDK12 inhibitor (antagonist) with IC50 of 0.641 μM at high ATP (2 mM). |
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V52286 | CDK12-IN-5 | 2651200-35-8 | CDK12-IN-5, a pyrazotriazine, is a potent CDK12 inhibitor (antagonist) with IC50 of 23.9 nM at high ATP (2 mM). |
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V52285 | CDK12-IN-6 | 2651196-71-1 | CDK12-IN-6 is a pyrazotriazine and a potent CDK12 inhibitor (antagonist) with IC50 of 1.19 μM at high ATP (2 mM). |
|
V55098 | CDK2-IN-13 | 101622-53-1 | CDK2-IN-13 (Compound 15) is a CDK2 inhibitor (antagonist) with IC50 of 12 µM. |
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V55091 | CDK2-IN-14 | 2862836-22-2 | CDK2-IN-14 (compound 4f) is a selective CDK2 inhibitor that may be utilized in cancer-related research. |
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V55082 | CDK2-IN-14-d3 | 2498658-25-4 | CDK2-IN-14-d3 is a potent and specific CDK2 inhibitor. |
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V55099 | CDK2-IN-15 | 1219915-83-9 | CDK2-IN-15 (Compound 19) is an inhibitor (blocker/antagonist) of CDK2 with IC50 of 2.9 μM. |
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V79856 | CDK2-IN-19 | CDK2-IN-19 (Compound 32) is a selective, orally bioactive CDK2 inhibitor (Ki: 0.18 nM). | |
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V78698 | CDK2-IN-20 | CDK2-IN-20 is an inhibitor (blocker/antagonist) of CDK2. | |
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V55071 | CDK2-IN-3 | 222035-13-4 | CDK2-IN-3 (compound 3) is a potent and specific CDK2 inhibitor at 50 and 60 nM. |
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V55097 | CDK2-IN-7 | 2498658-13-0 | CDK2-IN-7 is a CDK2 inhibitor (IC50 < 50 nM) for cancer research. |
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V75988 | CDK2-IN-8 | 2919216-36-5 | CDK2-IN-8 is a potent CDK2 inhibitor (antagonist) with IC50 of 1.74 µM. |
|
V75989 | CDK2-IN-9 | 2919216-33-2 | CDK2-IN-9 is a potent CDK2 inhibitor (antagonist) with IC50 of 0.63 µM. |
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V52283 | CDK2/4/6-IN-1 | 2803837-13-8 | CDK2/4/6-IN-1 (example 29) is a CDK2/4/6 inhibitor (antagonist) with IC50s of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6 respectively, may be utilized in cancer research. |
|
V55105 | CDK2/4/6-IN-2 | 2531748-80-6 | CDK2/4/6-IN-2 is a CKD2/4/6 inhibitor (antagonist) with IC50s: less than 1 μM, less than 10 nM, and less than 100 nM. |
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