GSK2850163 是新型的肌醇需要酶-1α (IRE1α) 抑制剂，抑制 IRE1α 激酶活性的IC50为 20nM，对 RNA 酶活性也有抑制活性，IC50为200 nM。

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).

The increased autophosphorylation of IRE1α could be reduced in a dose-dependent manner by GSK2850163. Increasing concentrations of GSK2850163 are capable of reducing the increased XBP 1 transcriptional activity. Two additional kinases are weakly inhibited by GSK2850163: Ron (IC50=4.4 μM) and FGFR1 V561M (IC50=17 μM).

2121989-91-9

C24H29Cl2N3O

446.41

Ethanol:50 mg/mL (112.00 mM),Need ultrasonic
DMSO:67.5 mg/mL (151.21 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years