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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-U4-I05
U4-I05

Chemical Structure : U4-I05

CAS No.: 956941-31-4

U4-I05 (ZINC000008877313)

货号: PC-23952Not For Human Use, Lab Use Only.

U4-I05 is a specific small molecule USP4 inhibitor (KD=239 nM) that inhibits USP4 deubiquitinating enzyme activity, inhibits stemness characteristics in CRC cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

U4-I05 is a specific small molecule USP4 inhibitor (KD=239 nM) that inhibits USP4 deubiquitinating enzyme activity, inhibits stemness characteristics in CRC cells.
U4-I05 inhibited CD44 protein expression in organoids derived from MC38 cells.
U4-I05 significantly suppressed tumorsphere formation and reduced the proportion of CD44+EpCAM+Lgr5+ cells, with no effects on stemness in cells with USP4 knockdown.
U4-I05 inhibits the protein expression of Twist1 and β-catenin by abolishing the deubiquitinating enzyme activity of USP4, thereby promoting protein degradation.
U4-I05 enhances the sensitivity of tumor cells to oxaliplatin.
U4-I05 exerts a potent anti-tumor effect by downregulating Twist1 and β-catenin expression and enhancing the sensitivity of tumor cells to oxaliplatin in xenograft mice.

物理化学性质&存储条件

分子量 498.54
分子式 C29H26N2O6
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

(1S,5R)-3-(2-((4-(4-methoxyphenyl)-2-oxo-2H-chromen-7-yl)oxy)acetyl)-1,2,3,4,5,6-hexahydro-8H-1,5-methanopyrido[1,2-a][1,5]diazocin-8-one

参考文献

1. Li F, et al. J Transl Med. 2025 Jan 24;23(1):114.

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