tcsc0040332 GSK2850163 hydrochloride

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Product Description

GSK2850163 hydrochloride 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.

IC50 & Target: IC50: 20 nM (IRE1α kinase activity), 200 nM (IRE1α RNase activity)[1]

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

Information

FormulaC24H30Cl3N3O
Clinical Informationclinicalinformation
PathwayCell Cycle/DNA Damage
TargetIRE1

Specifications

Purity / Grade>98%
Solubility10 mM in DMSO
Smilessmiles

Misc Information

Observed Molecular Weight482.87
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