ire1α kinase

KIRA-7 is an imidazopyrazine compound. KIRA-7 has an anti-fibrotic effect. KIRA-7 binds the IRE1α kinase (IC50: 110 nM) to allosterically inhibit its RNase activity.

IRE1α kinase-IN-5 (compound 7) is a potent ATP-competitive inhibitor of IRE1α with a Ki value of 98 nM.

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

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

IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM.

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

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-8, a benzoheterocyclecarboxaldehyde derivative, is a potent inhibitor of IRE-1α used in research on diseases related 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 with an average IC50 value of less than 0.1 μM, and it is suitable for research into diseases related to the unfolded protein response or regulated IRE1-dependent decay (RIDD) [1].

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

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α), effectively inhibiting both its RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).

Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.

Sunitinib (SU 11248) glucuronate is a multi-target receptor tyrosine kinase inhibitor with IC50 values of 80 nM for VEGFR2 and 2 nM for PDGFRβ. As an ATP-competitive inhibitor, it effectively suppresses Ire1α phosphorylation by inhibiting autophosphorylation and subsequent RNase activation.

GP17 is a type II kinase inhibitor of the IRE1α endoribonuclease that acts by targeting the ATP-binding pocket of IRE1α.

GP29 is a Type II kinase inhibitor of the IRE1α endoribonuclease that acts by targeting the ATP-binding pocket of IRE1α.

GSK2850163 hydrochloride is a novel inositol-requiring enzyme-1α (IRE1α) inhibitor that inhibits the kinase (IC50: 20 nM) and RNA enzyme (IC50: 200 nM) activities of IRE1α.

KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.