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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V81227 | PROTAC CDK9 degrader-8 | PROTAC CDK9 degrader-8 (compound 21) is a potent PROTAC CDK9 degrader with IC50 of 0.01 μM. | |
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V78300 | PROTAC CDK9/CycT1 Degrader-2 | 3020773-91-2 | PROTAC CDK9/CycT1 Degrader-2 is an inhibitor (blocker/antagonist) of CDK9 with IC50 of 45 nM. |
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V81230 | PROTAC FLT3/CDK9 degrader-1 | PROTAC FLT3/CDK9 degrader-1 is a potent dual PROTAC degrader of FLT3 and CDK9. | |
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V55081 | PSTAIR | 126675-53-4 | PSTAIR is a monoclonal antibody (mAb) that recognizes the PSTAIR sequence in Cdc28. |
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V1540 | Purvalanol A (NG60) | 212844-53-6 | Purvalanol A (NG60; NG-60; NG 60) is a potent and cell-permeable CDK (cyclin-dependent kinase) inhibitor with potential antitumor activity. |
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V13387 | Purvalanol B (NG 95) | 212844-54-7 | Purvalanol B (formerly known as NG-95) is a potent and selectivecyclin-dependent kinase (CDK) inhibitor, inhibiting Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p35, and Cdk2/cyclin B (IC50s = 6, 9, 6, and 6 nM, respectively. |
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V85825 | PYRA-2 | ||
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V55076 | QR-6401 | 2845096-18-4 | QR-6401 is an orally bioactive and selective macrocyclic CDK2 inhibitor (antagonist) with IC50s of 0.37, 10, and 22 for CDK2/E1, CDK9/T1, CDK1/A2, CDK6/D3, and CDK4/D1, respectively. |
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V53173 | rel-(2S,3R)-Voruciclib hydrochloride | 1253647-46-9 | rel-(2S,3R)-Voruciclib HCl is an isomer of Voruciclib HCl. |
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V3208 | RGB-286638 2HCl | 784210-87-3 | RGB-286638 2HCl, the dihydrochloride salt of RGB-286638, is a multi-targeted cyclin-dependent kinase (CDK) inhibitor. |
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V2853 | RGB-286638 free base | 784210-88-4 | RGB-286638 is a multi-targeted cyclin-dependent kinase (CDK) inhibitor. |
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V55066 | Ribociclib-d6 (LEE011-d6) | 1328934-40-2 | Ribociclib-d6 is a deuterated form of Ribociclib. |
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V76556 | Ribociclib-d6 hydrochloride (LEE011-d6 (hydrochloride)) | Ribociclib-d6 ( HCl) is a deuterated form of Ribociclib. | |
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V56539 | Ribociclib-d8 (LEE011-d8) | 2167898-24-8 | Ribociclib-d8 is the deuterium labelled form of Ribociclib. |
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V38370 | Rintodestrant (G1T48) | 2088518-51-6 | Rintodestrant (G1T48) is an orally bioactive, nonsteroidal, selective estrogen receptor degrader. |
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V6968 | Riviciclib HCl (P276-00) | 920113-03-7 | Riviciclib HCl (P276-00) is a flavonoid analog which acts as a novel inhibitor of CDK1 (cyclin-dependent kinase), CDK4 and CDK9 with IC50 of 79 nM, 63 nM and 20 nM, respectively. |
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V1541 | Ro-3306 | 872573-93-8 | RO-3306 (RO3306; RO 3306) is a novel, potent, ATP-competitive, and selective CDK1 inhibitor with potential antineoplastic activity. |
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V91065 | Roccellic acid | 29838-46-8 | Roccellic acid is a methanol extract of Roccella montagnei, which is cytotoxic with an IC50 value of 71.26 μg/ml. |
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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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