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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Nur77 (NR4A1)-4-PQBH
4-PQBH

Chemical Structure : 4-PQBH

CAS No.: 2765240-30-8

4-PQBH (4 PQBH)

货号: PC-21508Not For Human Use, Lab Use Only.

4-PQBH is a small molecule Nur77-mediated cytoplasmic vacuolation and paraptosis inducer, binds to Nur77 (KD=1.17 uM) and shows potentially selective cytotoxicity to HCC cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

4-PQBH is a small molecule Nur77-mediated cytoplasmic vacuolation and paraptosis inducer, binds to Nur77 (KD=1.17 uM) and shows potentially selective cytotoxicity to HCC cells.
4-PQBH extensively induces caspase-independent cytoplasmic vacuolization and paraptosis through Nur77-mediated ER stress and autophagy.
4-PQBH exhibits potent anti-HCC activity (HepG2 cells, IC50=2.6 uM) and is low toxic to normal LO2 cells (IC50=17.32 uM).
4-PQBH effectively inhibits tumor growth in HepG2 xenografted model in immunodeficient mice.
4-PQBH targets Nur77 to endoplasmic reticulum (ER) and induces Nur77-mediated ER stress as well as autophagy, resulting in cytoplasmic vacuolation and paraptosis-like cell death.

物理化学性质&存储条件

分子量 367.41
分子式 C22H17N5O
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

(E)-N'-(pyridin-4-ylmethylene)-4-(quinolin-4-ylamino)benzohydrazide

参考文献

1. Baicun Li, et al. Bioorg Chem. 2022 Apr:121:105651.

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