Synonyms: (S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide; 2-Chloro-N-[6-methyl-5-[[3-[2-[(3S)-3-piperidinylamino]-4-pyrimidinyl]-2-pyridinyl]oxy]-1-naphthalenyl]benzenesulfonamide; AMG 18; AMG-18; AMG18; Compound 18; IRE1alpha Kinase-Inhibiting RNase Attenuator 8
Molecular Formula: C31H29ClN6O3S
Molecular Weight: 601.12
Linear Structural Formula: C31H29ClN6O3S
MDL Number: MFCD28404657
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: KIRA8 is an ATP-competitive, potent and selective IRE1alpha kinase inhibitor (IRE1alpha/beta Ki = 2/120 nM) that attenuates IRE1alpha endonuclease activity (IRE1alpha/beta 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.).