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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V34732 | Manzamine A hydrochloride (Keramamine A hydrochloride) | 104264-80-4 | Manzamine A HCl is an orally bioactive β-carboline alkaloid that can inhibit GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM. |
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V4641 | Mevociclib (SY-1365) | 1816989-16-8 | Mevociclib (formerly SY-1365; SY1365) is a novel, potent, highly selective and covalent/irreversible inhibitor ofCDK7 (Cyclin-dependent kinase 7) with anticancer activity. |
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V1556 | Milciclib (PHA-848125) | 802539-81-7 | Milciclib (formerly also known as PHA-848125; PHA-848125AC; PHA848125) is a novel, potent, ATP-competitive small molecule CDK inhibitor with potential anticancer activity. |
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V55104 | ML 315 | 1440251-53-5 | ML 315 is a dual selective inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM respectively. |
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V1545 | ML167 (CID 44968231) | 1285702-20-6 | ML167 (also called CID-44968231; NCGC-00188654; ML-167; CID 44968231; NCGC00188654) is a novel, ATP-competitive and highly selective Cdc2-like kinase 4 (Clk4) inhibitor with potential anticancer activity. |
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V2742 | MSC2530818 | 1883423-59-3 | MSC2530818 is novel,potent, selective and orally available small molecule inhibitor of cyclin dependent kinase CDK8 with theIC50of 2.6 nM. |
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V76712 | NecroIr1 | NecroIr1 is an iridium(III) complex and a necrosis inducer in Cisplatin-resistant lung cancer cells (A549R). | |
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V76711 | NecroIr2 | NecroIr2 is an iridium(III) complex and a necrosis inducer in Cisplatin-resistant lung cancer cells (A549R). | |
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V5257 | NG 52 | 212779-48-1 | NG 52 (NG-52), a tri-substituted purine, is a cell-permeable, reversible, and ATP-competitve inhibitor of the cell cycle-regulating kinase, Cdc28p with IC50 of 7 μM, and the related Pho85p kinase with IC50 of 2 μM. |
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V0078 | NU2058 | 161058-83-9 | NU2058 (also known as NU 2058; NU-2058; O6-(Cyclohexylmethyl)guanine) is a novel and potent O(6)-Cyclohexylmethylguanine-based CDK2 (cyclin-dependent kinases 2) inhibitor with IC50 of 17 μM in an enzymatic assay. |
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V1546 | NU6027 | 220036-08-8 | NU6027 (NU-6027; NU 6027) is a novel, potent and ATP competitive ATR/CDK (ataxia telangiectasia and Rad3-related/Cyclin-dependent kinases) inhibitor with potential antitumor activity. |
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V26765 | NU6140 | 444723-13-1 | NU6140 is a selective CDK2-cyclin A inhibitor (IC50, 0.41 μM), which is 10-36 times more selective than other CDKs. |
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V4538 | NVP-LCQ-195 | 902156-99-4 | NVP-LCQ195 (formerly also known as AT9311; AT-9311; LCQ195; LCQ-195) is a novel and potent small molecule heterocyclic inhibitor of cyclin-dependent kinases CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM. |
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V41070 | ODN BW001 | 886862-38-0 | ODN BW001 is an oligonucleotide. |
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V80995 | ODN BW001 sodium | ODN BW001 sodium is an oligonucleotide. | |
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V5210 | Olomoucine | 101622-51-9 | Olomoucine,a purine derivative, is a novel and potent CDK (cyclin-dependent kinases) inhibitor that competes for the ATP binding site of the kinase and induces G arrest. |
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V3820 | ON-013100 | 865783-95-5 | ON-013100 is a novel and potent inhibitor of cell cycle with the potential for the treatment of mantle cell lymphoma. |
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V2823 | ON123300 | 1357470-29-1 | ON123300 is a novel,low molecular weight and potentmultikinase inhibitor identified through a series of screens that supported further analyses for brain tumor chemotherapy. |
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V3044 | Palbociclib (PD-0332991) | 571190-30-2 | Palbociclib (formerly PD-0332991; PD0332991; Pfizer trade nameIbrance) is a highly selective, orally bioavailable pyridopyrimidine-based CDK4/6 inhibitor that has been approved for cancer treatment. |
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V1531 | Palbociclib (PD-0332991) HCl | 827022-32-2 | Palbociclib HCl (Pfizer trade name Ibrance, also known as PD-0332991), the HCl salt of Palbociclib, is a highly selective, orally bioavailable pyridopyrimidine-derived inhibitor of CDK4/6 with potential antineoplastic activity. |
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