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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V5014 | THZ2 | 1604810-84-5 | THZ2, aTHZ1 analog, is a novel, potent and selective CDK7 inhibitor with an IC50 of 13.9 nM. |
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V4923 | THZ531 | 1702809-17-3 | THZ531 (THZ-531) is a novel, potent and irreversible / covalent inhibitor of Cyclin-dependent kinases CDK12 and CDK13 (IC50 =158 nM and 69 nM for CDK12/13, respectively) with anticancer effects. |
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V55078 | tibremciclib | 2397678-18-9 | Tibremciclib is a CDK4 inhibitor (antagonist) with anti-tumor activity. |
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V35177 | TP-1287 | 2044686-42-0 | TP-1287 is the prodrug of Alvocidib, an orally bioactive CDK9 inhibitor. |
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V83219 | TP-353 | 1253799-29-9 | TP-353 (EOS61973) is a novel and potent CDK7 inhibitor. |
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V16810 | Trilaciclib (G1T28) | 1374743-00-6 | Trilaciclib (G-1T28; G1T28; Cosela) is a novel, first-in-class and short-acting CDK4/6 inhibitor approved in 2021 by FDA as a medication to reduce the frequency of chemotherapy-induced bone marrow suppression. |
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V31977 | Trilaciclib hydrochloride (G1T28) | 1977495-97-8 | Trilaciclibhydrochloride (G-1T28; Cosela), the hydrochloride salt ofTrilaciclib, is a short-acting CDK4/6 inhibitor with anticancer activity. |
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V35145 | Vanicoside B | 155179-21-8 | Vanicoside B is a phenylpropyl sucrose analogue that can be extracted from Polygonum multiflorum (Persicaria dissitiflora). |
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V28036 | Voruciclib | 1000023-04-0 | Voruciclib (formerly known as P1446A-05) is a potent and orally bioavailable CDK4/cyclin-dependent kinase 4 inhibitor with potential anticancer activity. |
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V1543 | XL413 (BMS-863233) HCl | 1169562-71-3 | XL413 HCl (XL-413; BMS863233; XL 413; BMS-863233), the hydrochloride salt of XL413, is a novel and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antitumor activity. |
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V35116 | XL413 hydrochloride (BMS-863233 hydrochloride) | 2062200-97-7 | XL413 (BMS-863233) HCl is a specific, ATP-competitive inhibitor of Cdc7 with IC50 of 3.4 nM. |
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V75980 | XPW1 | 2700286-66-2 | XPW1 is a potent and specific CDK9 inhibitor (antagonist) with excellent activity against clear cell renal cell carcinoma (ccRCC) and low toxicity. |
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V41716 | YKL-5-124 | 1957203-01-8 | YKL-5-124 (YKL-5124) is a novel,selective, and covalent CDK7 inhibitor (IC50=53.5 nM) with anticancer activity. |
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V75986 | YKL-5-124 TFA | 2748220-93-9 | YKL-5-124 TFA is a specific and irreversible covalent inhibitor of CDK7 with IC50 of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. |
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V35105 | YX-2-107 | 2417408-46-7 | YX-2-107 is a PROTAC that selectively degrades CDK6 (IC50= 4.4 nM). |
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V75883 | ZLHQ-5f | 2851977-85-8 | ZLHQ-5f is a dual (bifunctional) inhibitor of CDK2 and Topo I, with IC50 of 0.145 μM for CDK2/CycA2. |
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V71683 | ZLMT-12 | 2841473-39-8 | ZLMT-12 (compound 35) is a tacnin analogue and a potent CDK2/9 inhibitor. |
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V75990 | ZLWT-37 | 2813347-44-1 | ZLWT-37 is a potent, orally bioactive CDKs inhibitor (antagonist) with IC50s of 0.002 μM and 0.054 μM for CDK9 and CDK2, respectively. |
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V73441 | ZNL-05-044 | ZNL-05-044 is a CDK11 inhibitor (antagonist) with IC50s of 0.23 μM and 0.27 μM for CDK11A and CDK11B, respectively, in NanoBRET experiments. | |
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V7667 | Zotiraciclib (TG-02, SB-1317) | 1204918-72-8 | Zotiraciclib (formerly TG02, SB1317) isan orally bioavailable, brain penetrant and multi-kinase (CDK/JAK2/FLT3) inhibitor for the treatment of cancer (e. |
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