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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V1557 | Palbociclib (PD0332991) Isethionate | 827022-33-3 | Palbociclib Isethionate (formerly known as PD0332991; PD-0332991; Ibrance), the isethionate salt of Palbociclib, is an orally bioavailable pyridopyrimidine-based inhibitor of CDK4/6 with potential antitumor activity and was approved as an anticancer drug. |
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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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V75991 | Palbociclib orotate (PD 0332991 orotate) | 2757498-64-7 | Palbociclib (PD 0332991) orotate 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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V0062 | PHA-767491 | 845714-00-3 | PHA-767491 (formerly also called CAY10572) is a novel and potent ATP-competitive dual inhibitor of Cdc7/CDK9 with IC50 of 10 nM and 34 nM in cell-free assays, respectively. |
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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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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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V0080 | Prexasertib 2HCl (LY-2606368) | 1234015-54-3 | Prexasertib 2HCl (also known as LY2606368) is the dihydrochloride salt of Prexasertib with potential anticancer activity. |
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V0079 | Prexasertib mesylate (LY-2606368 mesylate) | 1234015-55-4 | Prexasertib mesylate (also known as LY2606368 mesylate) is a novel, potent, selective and ATP competitive inhibitor of the CHK1 (checkpoint kinase 1) protein kinase with potential anticancer activity. |
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V0081 | Prexasertib mesylate hydrate (LY 2606368) | 1234015-57-6 | Prexasertib mesylate hydrate (also known as LY2606368 mesylate hydrate) is the hydrated mesylate salt of Prexasertib with potential anticancer activity. |
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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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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 | 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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