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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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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V89624 | Olomoucine II | 500735-47-7 | Olomoucine II is a potent CDK inhibitor with IC50 values of 0.06, 0.1, 0.45, 7.6 and 19.8 µM for CDK9/cyclin T, CDK2/cyclin E, CDK7/cyclin H, CDK1/cyclin B, CDK4/cyclin D1, respectively. |
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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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V87199 | P-gp/CDK2-IN-1 | P-gp/CDK2-IN-1 (Compound 4j) is an inhibitor of P-glycoprotein (P-gp) and cyclin-dependent kinase-2 (CDK2). | |
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V41051 | Palbociclib hydrochloride (PD-0332991 hydrochloride) | 571189-11-2 | Palbociclib (PD 0332991) HCl is an orally bioactive CDK4 and CDK6 selective inhibitor (antagonist) with IC50s of 11 nM and 16 nM, respectively. |
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V79067 | Palbociclib-d4 hydrochloride (PD 0332991-d4 (hydrochloride)) | Palbociclib-d4 ( HCl) is the deuterated form of Palbociclib HCl. | |
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V2832 | PHA-767491 HCl | 942425-68-5 | PHA-767491 HCl (formerlyknown as CAY10572 HCl) is a novel potent ATP-competitive and dual CDC7/CDK9 inhibitor with IC50 of 10 nM and 34 nM in cell-free assays, respectively. |
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V1552 | PHA-793887 | 718630-59-2 | PHA-793887 (PHA793887; PHA 793887) is a novel and ATP-competitive inhibitor of the multi-CDK (cyclin dependent kinases) for CDK2, CDK5 and CDK7 with potential anticancer activity. |
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V100248 | PKCζ-IN-1 | 1132609-87-0 | PKCζ-IN-1 is a compound that inhibits PKCζ and CDK2, with IC50 values of 5.18 nM for PKCζ and 1.04 μM for CDK2, showing obvious selectivity with a selectivity ratio of 200 times. |
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V2744 | Prexasertib (LY2606368) | 1234015-52-1 | Prexasertib (also known as LY2606368) is a novel, potent, selective and ATP competitive inhibitor of the CHK1 (checkpoint kinase 1) protein kinase with IC50 values of<1 nM and 8 nM for CHK1 and CHK2, respectively. |
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V76596 | PROTAC CDK12/13 Degrader-1 TFA | PROTAC CDK12/13 Degrader-1 (7f) TFA is a potent and specific cyclin-dependent kinase CDK12/CDK13 dual degrader with DC50s of 2.2 nM and 2.1 nM respectively. | |
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V55090 | PROTAC CDK9 degrader-2 | 2435721-30-3 | PROTAC CDK9 degrader-2 is a highly efficient and selective CDK9 degrader based on PROTAC technology. |
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V40836 | PROTAC CDK9 degrader-5 | 2935587-89-4 | PROTAC CDK9 degrader-5 is a PROTAC that specifically targets CDK9. |
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V40810 | PROTAC CDK9 degrader-6 | 2935587-91-8 | PROTAC CDK9 degrader-6 is a PROTAC that specifically targets CDK9. |
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V40695 | PROTAC CDK9 degrader-7 | 2935587-90-7 | PROTAC CDK9 degrader-7 is a PROTAC that specifically targets CDK9. |
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