IXA62 is an orally active and selective IRE1/XBP1s activator (EC50 = 0.31 μM) that reduces Aβ secretion. IXA62 enhances glucose-stimulated insulin secretion from rat insulinoma cells.

1ACTA is an IRE1α S-Nitrosylation inhibtor, maintaining the endoplasmic reticulum stress response under nitrosative stress.

TC-D-F07 is a novel prodrug of the covalent IRE-1 inhibitor D-F07, inhibits IRE-1/XBP-1s pathway in cancer cells.

PAIR1 is a partial antagonist of IRE1α RNase (PAIR) that fully engage IRE1α's kinase domain (Ki=220 nM) but only partially inhibit its RNase activity.

D-F07 is a novel fluorescent, covalent IRE-1 inhibitor, potently inhibits XBP-1s expression in MM cells.

APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.

STF-083010 is a specific IRE1α endonuclease inhibitor.

MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.

4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.

PAIR2 is a potent and selective partial antagonist of IRE1α RNase. PAIR2 can completely occupy IRE1α’s ATP-binding site in cells and block the ability of a potent KIRA to inhibit XBP1 splicing.

KIRA9 is a potent IRE1 inhibitor (IC50=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis.

A novel potent IRE1α-selective kinase inhibitor that inhibits both the kinase and RNase activities of IRE1α with IC50 of 20 nM and 200 nM, respectively; binds to pIRE1α and inhibits XBP 1 splicing; only weakly inhibits Ron (IC50= 4.4 uM) and FGFR1 V561M (IC50=17 uM) in a panel of 284 kinases.

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