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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-CDKL3 inhibitor HZ1
CDKL3 inhibitor HZ1

Chemical Structure : CDKL3 inhibitor HZ1

CAS No.: 3030492-40-8

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CDKL3 inhibitor HZ1 (C3I-22)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 362.44
分子式 C20H22N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-(4-((4-((3-cyclopentyl-1H-pyrazol-5-yl)amino)pyrimidin-2-yl)amino)phenyl)ethan-1-one

参考文献

1. Zhang H, et al. J Clin Invest. 2024 Jul 4:e178428.

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