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CDK9 degrader PO-8

Chemical Structure : CDK9 degrader PO-8

CAS No.:

CDK9 degrader PO-8

货号: PC-25541Not For Human Use, Lab Use Only.

CDK9 degrader PO-8 is a potent, selective iCDK9-based PROTAC degrader of CDK9 with DC50 of 0.26 uM in RAW 264.7 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CDK9 degrader PO-8 is a potent, selective iCDK9-based PROTAC degrader of CDK9 with DC50 of 0.26 uM in RAW 264.7 cells.
PO-8 does not affect CDKs (CDK1, CDK2, CDK4, CDK6, and CDK7).
PO-8′s degradation mechanism relies on CRBN-mediated ubiquitination.
PO-8 exhibits dose-dependent inhibition of LPS-induced inflammation in RAW264.7 cells.
PO-8 suppresses the JAK2-STAT3 signaling pathway by degrading CDK9
PO-8 (5-10 mg/kg) attenuates LPS-induced acute lung injury in LPS-induced murine acute lung injury (ALI) model, robustly suppresses LPS induced a pronounced upregulation of pro-inflammatory cytokines such as IL-6, IL-1β, and TNF-α.

物理化学性质&存储条件

分子量 823.37
分子式 C44H48ClFN8O5
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

N-((1r,4r)-4-((5'-chloro-6-((3-fluorobenzyl)amino)-[2,4'-bipyridin]-2'-yl)amino)cyclohexyl)-8-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)octanamide

参考文献

1. Ao MT, et al. Biochem Pharmacol. 2025 Sep 19:117341.

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