4μ8C (also known as IRE1 Inhibitor III) is a potent and selective IRE1 Rnase inhibitor (IC50 = 76 nM) with the potential for metabolic diseases.

NSC95682 (6-Bromo-2-hydroxy-3-methoxybenzaldehyde), extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5, is a novel and potent IRE-1α inhibitor with an IC50 of 0.08 μM.

STF-083010 (formerly IRE1 Inhibitor I) is a novel and specific small-molecule inhibitor of IRE1α endonuclease.

KIRA6 (KIRA-6) is a novel, potent and ATP-competitive allosteric IRE1α inhibitor (IC50 of 0.6 µM) with anti-inflammatory and immune-modulating properties.

Kira8 (AMG18; Kira-8; AMG-18) is a potent and allosteric inhibitor of IRE1α kinase-inhibiting rnase attenuator (kira) with antifibrotic effects.

MKC3946 (MKC-3946) is a potent and soluble IRE1α RNase inhibitor that has potential anticancer activity.

GSK2850163 is a novel and potent inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.

IXA-4 is a highly selective, non-toxic IRE1/XBP1s activator.