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Home >> Signaling Pathways >> DNA Damage/DNA Repair >> CDK

CDK

<div class="colum_1 clearer"><p>CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. In fact, yeast cells can proliferate normally when their CDK gene has been replaced with the homologous human gene. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase.</p><p>There are around 20 Cyclin-dependent kinases (CDK1-20) known till date. CDK1, 4 and 5 are involved in cell cycle, and CDK 7, 8, 9 and 11 are associated with transcription.</p><p>CDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational. Most knowledge of CDK structure and function is based on CDKs of <i>S. pombe</i> (Cdc2), <i>S. cerevisia</i> (CDC28), and vertebrates (CDC2 and CDK2). The four major mechanisms of CDK regulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDK inhibitory subunits (CKIs).</p></div>

Targets for  CDK

Products for  CDK

  1. Cat.No. Product Name Information
  2. GC65346 THAL-SNS-032 THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN). THAL-SNS-032 Chemical Structure
  3. GC10840 THZ1 Covalent CDK7 inhibitor,potent and selective THZ1 Chemical Structure
  4. GC25996 THZ1 2HCl THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7. THZ1 2HCl Chemical Structure
  5. GC12642 THZ1 Hydrochloride CDK7 inhibitor THZ1 Hydrochloride Chemical Structure
  6. GC37786 THZ1-R A non-cysteine reactive derivative of THZ1 THZ1-R Chemical Structure
  7. GC13511 THZ2 CDK7 inhibitor THZ2 Chemical Structure
  8. GC16420 THZ531 CDK12 and CDK13 covalent inhibitor THZ531 Chemical Structure
  9. GC50484 TL 12-186 Multikinase degrading PROTAC TL 12-186 Chemical Structure
  10. GC34118 Trilaciclib (G1T28) Trilaciclib (G1T28) is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib (G1T28) Chemical Structure
  11. GC34087 Trilaciclib hydrochloride (G1T28 hydrochloride) Trilaciclib hydrochloride (G1T28 hydrochloride) (G1T28 hydrochloride) is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride (G1T28 hydrochloride) Chemical Structure
  12. GC45983 Voruciclib A pan-CDK inhibitor Voruciclib Chemical Structure
  13. GC65311 Voruciclib hydrochloride Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL). Voruciclib hydrochloride Chemical Structure
  14. GN10017 Wogonin Wogonin Chemical Structure
  15. GC18117 XL413 Cdc7 inhibitor XL413 Chemical Structure
  16. GC26084 XL413 (BMS-863233) XL413 (BMS-863233) is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with IC50 of 3.4 nM, showing 63-, 12- and 35-fold selectivity over CK2, Pim-1 and pMCM2, respectively. Phase 1/2. XL413 (BMS-863233) Chemical Structure
  17. GC13328 XL413 hydrochloride

    Cdc7 inhibitor

     XL413 hydrochloride Chemical Structure
  18. GC62701 XY028-133 XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK. XY028-133 Chemical Structure
  19. GC62139 XY028-140 XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells. XY028-140 Chemical Structure
  20. GC62294 YKL-5-124 YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status. YKL-5-124 Chemical Structure
  21. GC62112 Zotiraciclib Zotiraciclib Chemical Structure
  22. GC35021 [pSer2, pSer5, pSer7]-CTD TFA [pSer2, pSer5, pSer7]-CTD (TFA), a substrate for CDK7 (cyclin dependent protein kinase), is a phosphorylated polypeptide at ser2, ser5 and ser7 sites of RNA polymerase II carboxy-terminal domain (CTD). [pSer2, pSer5, pSer7]-CTD TFA Chemical Structure
  23. GC35022 [pThr3]-CDK5 Substrate [pThr3]-CDK5 Substrate is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate Chemical Structure

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