CHIR-99021盐酸盐 T2310L

Product Introduction
Bioactivity


英文名: CHIR-99021 HCl

描述: CHIR-99021 HCl (Laduviglusib HCl) 是GSK-3α/β的高效选择性抑制剂，IC50值分别为10 nM和6.7 nM。它对GSK-3表现出显著的选择性，对CDC2、ERK2和其他蛋白激酶的选择性超过500倍。此外，CHIR-99021 HCl 是Wnt/β-catenin信号通路的强大激活剂。此外，它在小鼠和人类胚胎干细胞中都表现出增强自我更新的能力。此外，拉杜维格西单盐酸盐诱导自噬[1][2][3]。

体外活性: Laduviglusib monohydrochloride inhibits human GSK-3β with K i values of 9.8 nM [1]. Laduviglusib monohydrochloride is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites. In vitro kinase assays expose that Laduviglusib monohydrochloride specifically inhibits GSK3β (IC 50 =~5 nM) and GSK3α (IC 50 =~10 nM), with little effect on other kinases [4]. In the presence of Laduviglusib monohydrochloride the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM Laduviglusib monohydrochloride with an IC 50 of 4.9 μM [2].

体内活性: In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) monohydrochloride rapidly reduces plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration [1]. Laduviglusib (2 mg/kg) monohydrochloride given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib monohydrochloride treatment significantly blocks crypt apoptosis and accumulation of p-H2AX + cells, and improves crypt regeneration and villus height. Laduviglusib monohydrochloride treatment increases Lgr5 + cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h [5].

存储条件: keep away from direct sunlight,store under nitrogenPowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 54.0 mg/mL (107.6 mM)
H2O : 6.4 mg/mL (12.8 mM)


关键字: CHIR-99021 HCl

相关产品: Citric acid trilithium salt tetrahydrate | BRD5648 | TCS 21311 | GSK-3β inhibitor 14 | GSK-3β inhibitor 12 | R547 | 1-Azakenpaullone | MBM-55 | ALSTERPAULLONE | GSK3-IN-1

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Neuronal Differentiation Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Highly Selective Inhibitor Library | Metabolism Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途