Uses
IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines[1].
Biological Activity
IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines[1].
IRE1α kinase-IN-2 (compound 3) inhibits XBP1 mRNA splicing, even during ER stress[1].
References
[1]. Wang L, Perera BG, Hari SB, et al. Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. Nat Chem Biol. 2012;8(12):982-989.
