IRE1

Inositol-requiring enzyme 1 (IRE1) is a bifunctional serine/threonine kinase and endoribonuclease that is a major mediator of the unfolded protein response (UPR) during endoplasmic reticulum (ER) stress. It represents a potential therapeutic target for a number of diseases associated with endoplasmic reticulum stress. IRE1 is the only identified ER stress sensor in yeast and essential for UPR in animals and plants. As an ER transmembrane protein, IRE1 monitors ER homeostasis through an ER luminal stress-sensing domain and triggers UPR through a cytoplasmic kinase domain and an RNase domain. Upon ER stress, IRE1 RNase is activated through conformational change, autophosphorylation, and higher order oligomerization. Mammalian IRE1 initiates diverse downstream signaling of the UPR either through unconventional splicing of the transcription factor Xbp-1 or and through posttranscriptional modifications via Regulated IRE1-Dependent Decay (RIDD) of multiple substrates.

Cat. No.	Product name	CAS No.	Purity
T14847	B I09	1607803-67-7	98%
T14847	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 ...
TQ0101	MKC3946	1093119-54-0	98%
TQ0101	MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.
T9564	IRE1α kinase-IN-1	2328097-41-0	98%
T9564	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 inhi...
T6681	STF-083010	307543-71-1	98%
T6681	STF-083010 is a selective inhibitor of the IRE1α endonuclease.
T6363	4μ8C	14003-96-4	98%
T6363	4μ8C(IC50=76 nM) is an effective and specific IRE1 Rnase inhibitor.
T11488	GSK2850163	2121989-91-9	98%
T11488	GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).
T9848	GSK2850163 (S enantiomer)	2309519-81-9	98%
T9848	GSK2850163 (S enantiomer) is the inactive enantiomer of GSK2850163. GSK2850163 is an novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1a).
T0374L	Sunitinib	557795-19-4	98%
T0374L	Sunitinib, a multi-targeted RTK inhibitor, is targeting PDGFRβ and VEGFR2 (Flk-1) with IC50 of 2 nM and 80 nM and also inhibits c-Kit.
T0374	Sunitinib Malate	341031-54-7	98%
T0374	Sunitinib is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
T17143	Toyocamycin	606-58-6	98%
T17143	Toyocamycin is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM). To...
T11762L	Kira8	1630086-20-2	98%
T11762L	Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).
T9349	IXA4	1185329-96-7	98%
T9349	IXA4 is a highly selective, nontoxic activator of IRE1/XBP1s and reduces APP secretion by activating IRE1. IXA4-stimulated IRE1 activation also enhanced pancreat...
T3654	APY29	1216665-49-4	98%
T3654	APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
TQ0076	KIRA6	1589527-65-0	98%
TQ0076	KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 µM). It can trigger an apoptotic response.
T12071	MKC9989	1338934-20-5	98%
T12071	MKC9989 is an inhibitor of Hydroxy aryl aldehydes (HAA). MKC9989 also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
T7483	6-Bromo-2-hydroxy-3-methoxybenzaldehyde	20035-41-0	98%
T7483	6-Bromo-2-hydroxy-3-methoxybenzaldehyde is an inhibitor of IRE-1α (IC50 : 0.08 μM).
T15594	MKC8866	1338934-59-0	98%
T15594	MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro). MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased productio...