PAIR2 is a selective inhibitor targeting the kinase domain of human IRE1α, exhibiting a Ki value of 8.8 nM. This compound effectively occupies the ATP-binding site, partially inhibiting IRE1α's ribonuclease activity while preserving Xbp1 mRNA splicing. PAIR2 also promotes the differentiation of B cells into plasma cells, prevents IRE1α-induced apoptosis, and restores Fgfr2 mRNA expression in AT2 cells. With its ability to reach steady-state concentrations in lung tissues of Mus musculus, PAIR2 is a valuable tool for exploring the role of the IRE1α signaling pathway in conditions such as pulmonary fibrosis.
PAIR2 is a selective inhibitor targeting the kinase domain of human IRE1α, exhibiting a Ki value of 8.8 nM. This compound effectively occupies the ATP-binding site, partially inhibiting IRE1α's ribonuclease activity while preserving Xbp1 mRNA splicing. PAIR2 also promotes the differentiation of B cells into plasma cells, prevents IRE1α-induced apoptosis, and restores Fgfr2 mRNA expression in AT2 cells. With its ability to reach steady-state concentrations in lung tissues of Mus musculus, PAIR2 is a valuable tool for exploring the role of the IRE1α signaling pathway in conditions such as pulmonary fibrosis.
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