KIRA8，5MG，SML2903-5MG，Sigma

Biochem/physiol Actions

ATP-competitive, potent and selective IRE1α kinase inhibitor that attenuates IRE1α endonuclease activity in vitro and in vivo.
KIRA8 is an ATP-competitive, potent and selective IRE1α kinase inhibitor (IRE1α/β K_i = 2/120 nM) that attenuates IRE1α endonuclease activity (IRE1α/β IC₅₀ = 5/55 nM) with good kinome selectivity. KIRA8 inhibits thapsigargin-induced UPR (IC₅₀ = 99 nM; HT1080 XBP1-Luc cells) and shows therapeutic efficacy in murine models of type 1 diabetes (T1D), pulmonary fibrosis, multiple myeloma (MM), and pancreatic neuroendocrine tumors (PanNET) in vivo (30-50 mg/kg/day i.p.).