IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM)

IRE1α kinase-IN-4 (compound 6) is a potent inhibitor of IRE1α, exhibiting a Ki value of 140 nM. It acts as an ATP-competitive ligand for IRE1α [1].

IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, serves as a potent inhibitor of IRE-1α. This compound is utilized in research pertaining to diseases linked to the unfolded protein response and regulated IRE1-dependent decay (RIDD) [1].

IRE1α kinase-IN-9 (compound 2) is a potent inhibitor of IRE-1α, demonstrating an average IC50 value of less than 0.1 μM. It is suitable for research into diseases linked to the unfolded protein response or regulated IRE1-dependent decay (RIDD) [1].

IRE1α kinase-IN-5 (compound 7) is a potent inhibitor of IRE1α (Ki: 98 nM) and is an ATP-competitive ligand for IRE1α.

IRE1α kinase-IN-2 is a highly potent inhibitor of IRE1α kinase, demonstrating an EC50 of 0.82 μM. It effectively impedes IRE1α kinase autophosphorylation with an IC50 of 3.12 μM. Additionally, IRE1α kinase-IN-2 effectively inhibits the splicing of XBP1 mRNA in wild-type cell lines.

IRE1α kinase-IN-7 is a chemical compound functioning as an inhibitor of IRE1α kinase, primarily utilized in the research of diseases related to endoplasmic reticulum stress.

IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC 50 value of 4.4 nM.

IRE1α kinase-IN-3 is a potent, ATP-competitive inhibitor of IRE1α (Ki: 480 nM).