产品描述:
APY-29 is a modulator of inositol requiring enzyme 1 α (IRE1α), which is a protein located in the endoplasmic reticulum (ER) membrane that has kinase and RNase activities triggered by ER stress.{36117} It binds to the ATP-binding site on IRE1α, where it inhibits its autophosphorylation (IC50 = 280 nM) and enhances its RNase function (EC50 = 460 nM). In vitro, it restores the ability of dephosphoylated IRE1α to cleave XBP1 mRNA in a dose-dependent manner. It also enhances IRE1α oligomerization in a crosslinking assay.