CAS:39122-38-8N-(Pyridin-2-yl)pyridine-2-carbothioamide

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NSC 185058 is an ATG4B inhibitor with IC50 of 3.24 µM.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

39122-38-8

储存条件

分子式

C11H9N3S

运输

蓝冰

分子量

215.27

别名

溶解度

DMSO	100.0 mg/mL (464.5 mM)
Water	insoluble

动物实验配方

生物活性

描述ATG4B, a substrate of mammalian sterile20-like kinase (STK) 26/MST4, stimulates autophagy by promoting autophagosome formation through reversible modification of ATG8. NSC185058 is a potent ATG4B inhibitor. NSC185058 at concentration ranging in 1-100μM dose-dependently inhibited starvation-induced autophagy, shown by GFP-labeled LC3 and fractional volumes of autophagic vacuoles in Saos-2 cells. It effectively suppressed the activation and lipidation of LC3B, as well as ATG4 activity. Administration of NSC185058 at dose of 100mg/kg inhibited starvation-induced autophagy in vivo and had a negative impact on the development of Saos-2 osteosarcoma tumors in immunodeficient nu/nu female mice injected subcutaneously with Saos-2 cells. NSC185058 decreased ATG4B-induced conversion of LC3-I to lipidated LC3-II, and the degradation of autophagy substrate p62/SQSTM1. It attenuated glioma stem-like cells growth and self-renewal, and enhanced the therapeutic effects of IR.
作用机制NSC185058 can bind to the pocket containing histidine 280 and aspartic acid 278, which are required for the proteolytic activity of ATG4B, through hydrophilic and hydrophobic binding interactions.^[1]
动物研究
剂量
Mice: 150 mg/kg^[2] (i.p.)

给药途径
i.p.