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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V1538 | Flavopiridol (Alvocidib) HCl | 131740-09-5 | Flavopiridol HCl(also known as Alvocidib; NSC 649890;HMR-1275; L-868275; HL-275;MDL-107,826A), the HCl salt of flavopiridol which is a flavanoid, is a broad spectrum and ATP-competitive inhibitor ofcyclin-dependent kinases-CDKs with potential antineoplastic activity. |
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V84915 | FMF-04-159-R | 2741262-15-5 | |
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V51480 | GP-82996 (CINK-4) | 359886-84-3 | GP-82996 (CINK-4) is a selective CDK4/6 pharmacological inhibitor. |
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V83861 | GPX4/CDK-IN-1 | ||
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V52032 | GSK-3 inhibitor 3 | 2227279-84-5 | GSK-3 inhibitor 3 is a selective, orally bioactive and brain-penetrating inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. |
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V52031 | GSK-3 inhibitor 4 | 2227279-83-4 | GSK-3 inhibitor 4 is an orally bioactive and brain-penetrating inhibitor of GSK-3, CDK2 and CDK5, with IC50s of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α) and 0.47 μM, respectively. |
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V52026 | GW297361 | 388627-21-2 | GW297361 is an oxidized indole CDK inhibitor that induces Pho85-selective responses in cells. |
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V78765 | H1k | H1k is a Eudistomin Y analogue and a lysosome-targeting antiproliferation agent. | |
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V69714 | Haspin-IN-1 | 2768474-30-0 | Haspin-IN-1 (compound 2a) is a haspin inhibitor (antagonist) with IC50 of 119 nM. |
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V69708 | Haspin-IN-2 | 2768474-47-9 | Haspin-IN-2 (compound 4) is a potent and specific haspin inhibitor (antagonist) with IC50 of 50 nM. |
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V60081 | HDAC-IN-51 | HDAC-IN-51 is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10, HDAC1, HDAC2, HDAC3 and HDAC11, respectively | |
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V75839 | HDAC1/CDK7-IN-1 | 2987905-95-1 | HDAC1/CDK7-IN-1 (compound 8e) is a dual (bifunctional) inhibitor of CDK7 and HDAC1 with IC50 of 893 nM and 248 nM, respectively. |
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V4382 | HQ461 | 1226443-41-9 | HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. |
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V51970 | hSMG-1 inhibitor 11e | 1402452-10-1 | hSMG-1 inhibitor 11e is a potent and specific hSMG-1 kinase inhibitor (antagonist) with IC50 of <0.05 nM. |
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V24310 | hSMG-1 inhibitor 11j | 1402452-15-6 | hSMG-1 inhibitor 11j, a pyrimidine analogue, is a potent and specific hSMG-1 inhibitor (antagonist) with IC50 of 0.11 nM. |
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V51040 | Indirubin-3-oxime (IDR-3O) | 667463-82-3 | Indirubin-3′-oxime (IDR3O), a synthetic indirubin derivative, is a novel inhibitor of glycogen synthase kinase 3β (GSK3β) and cyclin-dependent kinases (CDKs). |
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V55077 | Inixaciclib | 2370913-42-9 | Inixaciclib is a potent CDK inhibitor that may be utilized in anti-cancer research. |
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V85794 | INX-315 | 2745060-92-6 | |
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V51944 | Ipivivint | 1481617-15-5 | Ipivivint (compound 38) is a potent CDC-like kinase (CLK) inhibitor (antagonist) with EC50s of 1 nM and 7 nM for CLK2 and CLK3, respectively. |
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V51930 | IV-361 | 2055741-39-2 | IV-361 is an orally bioactive, selective CDK7 inhibitor (Ki≤50 nM). |
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