SML2903

KIRA8

≥98% (HPLC)

• Synonym(s): (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, IRE1α Kinase-Inhibiting RNase Attenuator 8
• Empirical Formula (Hill Notation): C₃₁H₂₉ClN₆O₃S
• CAS Number: 1630086-20-2
• Molecular Weight: 601.12
• MDL number: MFCD28404657
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: [S](=O)(=O)(Nc2c3c(c(c(cc3)C)Oc4ncccc4c5nc(ncc5)N[C@@H]6CNCCC6)ccc2)c1c(cccc1)Cl
• InChI key: XMWUCMFVDXDRDE-NRFANRHFSA-N

Description

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.).

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3