纯度:97% by TLC;NMR (Conforms)
分子式:C11H8O4
分子量:204.18
溶剂:DMSO (20 mg/ml)
性状:Yellow solid
存储:-20°C
Activity (short version):IRE1 ribonuclease inhibitor
Function / Pharmacology:Selective inhibitor of IRE1α ribonuclease (RNase) activity (IC50 = 60 nM). Covalently binds to lysine 907 in the IRE1 endonuclease domain, blocking substrate access to the active site of IRE1α and inactivating both XBP1 splicing and IRE1α-mediated mRNA degradation but not IRE1 kinase activity1. Inhibits IRE1α in response to hypoxia or other ER stress-inducing agents but has no effect on proliferation or clonogenic survival of hypoxic cells2. Blocks production of IL-4, IL-5 and IL-13 production in T cells3. Prevents the splicing of the XBP1 mRNA in response to ER stress caused by mutant proinsulin production in pancreatic β-cells4.