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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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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V1559 | R547 (Ro 4584820) | 741713-40-6 | R547 (R-547;Ro4584820;R 547;Ro-4584820)is a potent, selective and ATP-competitive inhibitor of CDK1/2/4 with potential antitumor activity. |
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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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V1550 | Ribociclib (LEE011) | 1211441-98-3 | Ribociclib (formerly NVP-LEE011; LEE011; LEE-011; trade name:Kisqali) is a potent, orally bioavailable and highly specific inhibitor of CDK4/6 (cyclin-dependent kinase) with potential antineoplastic activity. |
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V3924 | Ribociclib HYDROCHLORIDE | 1211443-80-9 | Ribociclib HCl (formerly also known as LEE-011; NVP-LEE011; Kisqali), the hydrochloride salt ofRibociclib, is an orally bioavailable CDK4/6 (cyclin-dependent kinase) inhibitor (IC50s = 10 nM and 39 nM) approved in March 2017 by FDA to treat postmenopausal women with a type of advanced breast cancer. |
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V3925 | RIBOCICLIB SUCCINATE (LEE011) | 1374639-75-4 | Ribociclib succinate (LEE011; NVP-LEE-011; LEE-011, NVP-LEE011; Kisqali), the succinate salt of Ribociclib, is a CDK4/6 (cyclin-dependent kinase) inhibitor (IC50s = 10 nM and 39 nM) approved in March 2017 by FDA for the treatment of breast cancer. |
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V3926 | RIBOCICLIB SUCCINATE HYDRATE | 1374639-79-8 | Ribociclib succinate hydrate (LEE011; LEE-011; NVP-LEE-011; NVP-LEE011; Kisqali), the succinate salt and hydrated form of Ribociclib, is a potent inhibitor of CDK4/6 (cyclin-dependent kinase) (IC50s = 10 nM and 39 nM) approved in March 2017 by FDA for the treatment of breast cancer. |
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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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V1549 | Riviciclib (P276-00) | 920113-02-6 | Riviciclib (formerly P 276-00;P-27600;P276-00) is a flavonoid analog which acts as a potent inhibitor of CDK1 (cyclin-dependent kinase), CDK4 and CDK9 with potential antitumor activity. |
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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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V4211 | Roniciclib | 1223498-69-8 | Roniciclib (formerly also known as BAY1000394; BAY-1000394) is a novel, potent and orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor wwith anticancer activity. |
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