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Chemical Structure : CDKL3 inhibitor HZ1
Catalog No.: PC-22841Not For Human Use, Lab Use Only.
CDKL3 inhibitor HZ1 (C3I-22) is a first-in-class, specific inhibitor of CDKL3 (Cyclin-dependent kinase like 3) inhibitor with Kd of 5.16 uM, blocks CDKL3 mediated cell cycle progression both in vitro and in vivo
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CDKL3 inhibitor HZ1 (C3I-22) is a first-in-class, specific inhibitor of CDKL3 (Cyclin-dependent kinase like 3) inhibitor with Kd of 5.16 uM, blocks CDKL3 mediated cell cycle progression both in vitro and in vivo
C3I-22 (HZ1) exhibits potent tumor-suppressing effect with IC50 of 0.348 and 0.086 uM in U2OS and DLD-1 cells respectively.
C3I-22 (HZ1) antagonizes cancer growth via cell cycle arrest in multiple models, reduces the levels of pRb and CDK4.
C3I-22 (HZ1) could overcome the acquired drug resistance of CDK4/6 inhibitor in ER+ breast cancer.
C3I-22 (HZ1) could act on a different stage (G0-to-G1 transition) from CDK4/6 inhibitor and meanwhile suppress the elevated CDK4/6 protein level.
C3I-22 significantly reduced the tumor number and volume, efficiently clear the tumor burden derived from the colon cancer patient.
CDKL3 belongs to Cyclin-Dependent Kinase Like (CDKL) kinase subfamily, which is part of CMGC Ser/Thr protein kinase superfamily. Serine/Threonine kinase, CDKL3 (Cyclin-dependent kinase like 3), crucially drives the rapid cell cycle progression and cell growth in cancers.
| M.Wt | 362.44 | |
| Formula | C20H22N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Zhang H, et al. J Clin Invest. 2024 Jul 4:e178428.
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