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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V77146 | CLK1-IN-2 | CLK1-IN-2 is a metabolically stable Clk1 inhibitor. | |
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V52240 | CLK1-IN-3 | 2922550-28-3 | CLK1-IN-3 (compound 10ad) is a potent and specific Clk1 inhibitor (antagonist) with IC50 of 5 nM and is over 300-fold selective over Dyrk1A. |
|
V52224 | CPS2 | 2756741-90-7 | CPS2 is a highly efficient, selective, irreversible PROTAC CDK2 degrader (IC50= 24 nM). |
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V52217 | Crozbaciclib fumarate | 2567494-39-5 | Crozbaciclib fumarate is an inhibitor (blocker/antagonist) of CDK4/6 with IC50s of 3 and 1 nM respectively. |
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V18895 | CVT-313 | 199986-75-9 | CVT-313 (Cdk2 Inhibitor III) is a potent ATP-competitive and selective CDK2 inhibitor (antagonist) with IC50 of 0.5 μM. |
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V84503 | Cyclin K degrader 1 | ||
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V3317 | Dalpiciclib | 1637781-04-4 | Dalpiciclib (SHR-6390) is an orally bioactive and selective CDK4/6 inhibitor (antagonist) with IC50s of 12.4 nM and 9.9 nM, respectively. |
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V52200 | Dalpiciclib hydrochloride (SHR-6390 hydrochloride) | 2891598-76-6 | Dalpiciclib (SHR-6390) HCl is an orally bioactive and selective CDK4/6 inhibitor (antagonist) with IC50s of 12.4 nM and 9.9 nM, respectively. |
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V84683 | DB18 | 2587177-94-2 | |
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V53108 | DD-03-156 ((S,R,S)-AHPC-Me-PEG2-dabrafenib) | 2769753-69-5 | DD-03-156 is a potent and specific degrader of CDK17 and LIMK2. |
|
V1534 | Dinaciclib (SCH727965) | 779353-01-4 | inaciclib (formerly known as PS-095760, SCH727965; PS 095760; SCH 727965) is a novel, selective and potent cyclin-dependent kinases (CDK) inhibitor with potential antineoplastic activity. |
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V52936 | DS96432529 | 2871872-79-4 | DS96432529 is a potent bone anabolic agent with orally bioactive and CDK8 inhibitory activity. |
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V4452 | Ebvaciclib (PF-06873600) | 2185857-97-8 | Ebvaciclib (PF-06873600; PF06873600) is a novel, potent, selective and orally bioavailable pan-inhibitor of cyclin-dependent kinase (CDK) with potential antitumor activity. |
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V53301 | Eciruciclib | 1868086-40-1 | Eciruciclib is an anticancer agent and a potent cyclin-dependent kinase (CDK) inhibitor. |
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V52134 | EGFR/CDK2-IN-1 | 2841405-96-5 | EGFR/CDK2-IN-1 (compound 3b) is an EGFR/CDK2 inhibitor. |
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V79258 | EGFR/CDK2-IN-2 | EGFR/CDK2-IN-2 (compound 6a) is a dual (bifunctional) inhibitor of EGFR and CDK-2 with IC50s of 19.6 and 87.9 nM, respectively. | |
|
V79259 | EGFR/CDK2-IN-3 | EGFR/CDK2-IN-3 (compound 4b) is a dual (bifunctional) inhibitor of EGFR and CDK-2 with IC50s of 71.7 and 113.7 nM respectively. | |
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V79124 | EGFR/CDK2-IN-4 | EGFR/CDK2-IN-4 (compound 4c) is a dual (bifunctional) inhibitor of EGFR and CDK-2 with IC50s of 89.6 and 165.4 nM respectively. | |
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V41638 | FIT-039 | 1113044-49-7 | FIT-039 (FIT039) is an oral, selective and ATP-competitive CDK9 (cyclin-dependent kinase 9) inhibitor with antiviral activity. |
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V1535 | Flavopiridol (Alvocidib) | 146426-40-6 | Flavopiridol (also known as Alvocidib, NSC 649890 HCl;HMR1275;L868275; HMR 1274;NSC649890), a broad spectrum and ATP-competitive inhibitor ofCDKs with potential antineoplastic activity. |
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