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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-CDK9 inhibitor HS34
CDK9 inhibitor HS34

Chemical Structure : CDK9 inhibitor HS34

CAS No.:

CDK9 inhibitor HS34

货号: PC-26367Not For Human Use, Lab Use Only.

CDK9 inhibitor HS34 is a potent, selective CDK9 inhibitor with IC50 of 1.4 nM (CDK9/CycT1), shows 250-fold selectivity over CDK2/CycA2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CDK9 inhibitor HS34 is a potent, selective CDK9 inhibitor with IC50 of 1.4 nM (CDK9/CycT1), shows 250-fold selectivity over CDK2/CycA2.
HS34 shows potent and broad antiproliferative activity for MDA-MB-231 (GI50 = 0.22 μM) and 4T1 cells (GI50 = 0.53 μM).
HS34 (500 nM) inhibits CDK9 by 99.2%, demonstrating potent on-target activity.
HS34 effectively suppresses TNBC cell motility, inhibits the metastatic potential of TNBC cells.
HS34 suppresses RNAP II Ser2 phosphorylation, leading to the downregulation of short-lived survival and oncogenic proteins such as Mcl-1 and c-Myc, and consequently inducing apoptosis and blocking EMT-associated invasion.
HS34 (20 mg/kg, p.o.) demonstrated in vivo antitumor efficacy and mechanism-driven pharmacodynamics in TNBC models.

物理化学性质&存储条件

分子量 450.51
分子式 C25H27FN4O3
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

(R)-N-(5-Fluoro-4-(4-((S)-2-methylpyrrolidin-1-yl)-2-oxo-2H-chromen-6-yl)pyridin-2-yl)piperidine-3-carboxamide

参考文献

1. Huang Y, et al. J Med Chem. 2026 Mar 11. doi: 10.1021/acs.jmedchem.5c03822.

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