GSK-3抑制剂4 T77341

Product Introduction
Bioactivity


英文名: GSK-3 inhibitor 4

描述: GSK-3 inhibitor 4 是一种具有口服活性和脑渗透性的 GSK-3，CDK2 和 CDK5 三重抑制剂，对 GSK-3β，GSK-3α，CDK2 和 CDK5 具有抑制作用，IC50 值分别为 0.56 nM ，0.45 nM ，0.47 μM，0.68 μM。GSK-3 inhibitor 4 可有效降低 Tau protein 水平。GSK-3 inhibitor 4 可用于研究阿尔茨海默症 。

体外活性: GSK-3 inhibitor 4 (compound 40) is effective against CDK2 (840-fold, IC50 = 0.47 μM), CDK5 (1200-fold, IC50 = 0.68 μM), GSK-3β (IC50 = 0.56 nM), and GSK-3α (IC50 = 0.45 nM) exhibits excellent selectivity.[1]GSK-3 inhibitor 4 has good permeability and shows a high ability to bind to plasma proteins and brain tissue due to its lipophilicity.[1]

体内活性: GSK-3 inhibitor 4 (10 mg/kg; p.o.) reduced pTau396 by 37% when the nanosuspension was administered orally at a dose of 10 mg/kg.[1]GSK-3 inhibitor 4 (2 mg/kg, i.v.; 10 mg/kg, p.o.) exhibits low-moderate clearance, ranging from 15.8 to 23.3 mL/min/kg, and is well absorbed when administered orally as a solution.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (123.95 mM)


关键字: GSK3inhibitor4 | GSK-3 inhibitor 4

相关产品: RGB-286638 free base | GSK-3β inhibitor 12 | CDK8-IN-12 | MBM-55 | Bakkenolide A | GSK-3β inhibitor 11 | Bikinin | CHIR-99021 | (E/Z)-GSK-3β inhibitor 1 | CP21R7

相关库: Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Bioactive Compound Library

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