4μ8C (IRE1 Inhibitor III)(IC50=76 nM) is an effective and specific IRE1 Rnase inhibitor.

D-F07 is a novel fluorescent IRE-1 RNase inhibitor and a tricyclic chromone with potential anticancer activity.

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

Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycetes, functioning as an XBP1 inhibitor and inhibiting IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM), and induces apoptosis.

B I09, an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells.

IXA4 is a highly selective, nontoxic activator of IRE1/XBP1s and reduces APP secretion by activating IRE1. IXA4-stimulated IRE1 activation also enhanced pancreatic function.

STF-083010 is a selective inhibitor of the IRE1α endonuclease.

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).