PAIR2 is a highly selective inhibitor targeting the kinase domain of human IRE1alpha, with a Ki value of 8.8 nM against human IRE1alpha. PAIR2 fully occupies the ATP-binding site of the IRE1alpha kinase domain, partially antagonizes the ribonuclease activity of IRE1alpha, specifically inhibits regulated IRE1alpha-dependent decay (RIDD) and its mediated substrate cleavage, while preserving the splicing function of Xbp1 mRNA. PAIR2 also promotes the differentiation of B cells into plasma cells, blocks IRE1alpha-induced cell apoptosis, and restores the expression of Fgfr2 mRNA in AT2 cells. PAIR2 effectively reaches a steady-state concentration in the lung tissues of Mus musculus, and serves as an important tool for investigating the function of the IRE1alpha signaling pathway in diseases such as pulmonary fibrosis[1][2].
Molekulargewicht:
590.59
CAS Nummer:
[2771006-54-1]
Formel:
C27H26F4N6O3S
Target-Kategorie:
Apoptosis,FGFR,IRE1
Anwendungsbeschreibung:
MCE Product type: Reference compound
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