2771006-54-1
Chemical Structure
PAIR2
- CAS No.: 2771006-54-1
- Formula:C27H26F4N6O3S
- Molecular Weight:590.59
IUPAC Name: N-(methyl-d3)isonicotinamide
InChIKey: OIBXRLOQDGELGQ-KRWDZBQOSA-N
SMILES: CC(C(F)=C(NS(CC(F)(F)F)(=O)=O)C1=C2C=CC=C1)=C2OC3=NC=CC=C3C4=NC(N[C@H]5CCCNC5)=NC=C4
Biological Activity: PAIR2 is a highly selective inhibitor targeting the kinase domain of human IRE1α, with a Ki value of 8.8 nM against human IRE1α. PAIR2 fully occupies the ATP-binding site of the IRE1α kinase domain, partially antagonizes the ribonuclease activity of IRE1α, specifically inhibits regulated IRE1α-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 IRE1α-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 IRE1α signaling pathway in diseases such as pulmonary fibrosis[1][2].
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PAIR2 | PAIR2 is a highly selective inhibitor targeting the kinase domain of human IRE1α, with a Ki value of 8.8 nM against human IRE1α. PAIR2 fully occupies the ATP-binding site of the IRE1α kinase domain, partially antagonizes the ribonuclease activity of IRE1α, specifically inhibits regulated IRE1α-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 IRE1α-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 IRE1α signaling pathway in diseases such as pulmonary fibrosis. | |||||||||||||||||||||
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- [1]. Feldman HC, et al. ATP-competitive partial antagonists of the IRE1α RNase segregate outputs of the UPR. Nat Chem Biol. 2021;17(11):1148-1156. [Content Brief]
- [2]. Auyeung VC, et al. Pharmacologic inhibition of IRE1α-dependent decay protects alveolar epithelial identity and prevents pulmonary fibrosis in mice. J Clin Invest. 2025;135(20):e184522. Published 2025 Oct 15. [Content Brief]
Keywords
