GSK2850163 是一个新型的肌醇需要酶-1α (IRE1α) 抑制剂，它可抑制 IRE1α 的激酶活性和 RNA 酶活性，其 IC₅₀ 值分别为 20 和 200 nM。

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC 50 s of 20 and 200 nM, respectively.

Oil

IC50: 20 nM (IRE1α kinase activity), 200 nM (IRE1α RNase activity)

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively. 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). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Pure form -20°C 3 years；4°C 2 years

[1]. Nestor O. Concha, et al. Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity. Molecular Pharmacology December 2015, 88 (6) 1011-1023.

In Vitro: DMSO : 67.5 mg/mL (151.21 mM; Need ultrasonic)Ethanol : 50 mg/mL (112.00 mM; Need ultrasonic)配制储备液