IRE1

Inositol requiring enzyme 1

IRE1

Related Products

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.

IRE1 Related Products (71)
Recombinant Proteins (2)
Antibodies (2)

By Effects:	Inhibitors (54) Degraders (2) Antagonist (1) Activators (8) Modulator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-10255A

Sunitinib	Inhibitor	99.04%
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.

HY-19707

4μ8C	Inhibitor	99.95%
4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.

HY-15845

STF-083010	Inhibitor	98.0%
STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.

HY-139214

IXA4	Inhibitor	98.92%
IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1 activation.

HY-104040

MKC8866	Inhibitor	99.95%
MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC₅₀ of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC₅₀ of 0.52 μM and unstresses RPMI 8226 cells with an IC₅₀ of 0.14 μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.

HY-150280

Ironomycin	Activator
Ironomycin is a derivative of Salinomycin (HY-15597). Ironomycin exhibits selective inhibitory activity against mantle cell lymphoma (MCL) cells. Ironomycin blocks the cell cycle and induces apoptosis and ferroptosis. Ironomycin induces double-strand DNA breaks and activates the unfolded protein response (UPR), particularly the IRE1α signaling pathway accumulation. The combination of Ironomycin with Ibrutinib (HY-10997) shows a synergistic effect. Ironomycin can be used for the study of MCL.

HY-10255C

Sunitinib glucuronate	Inhibitor
Sunitinib (SU 11248) glucuronate is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib glucuronate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.

HY-180780

G1167	Degrader
G1167 is an IRE1 ligand, which can be used for the synthesis of PROTACs, such as G6374 (HY-180787).

HY-10255

Sunitinib Malate	Inhibitor	99.74%
Sunitinib (SU 11248) Malat is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malat, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.

HY-19708

KIRA6	Inhibitor	99.86%
KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC₅₀ of 0.6 µM. KIRA6 can trigger an apoptotic response.

HY-103248

Toyocamycin	Inhibitor	99.27%
Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC₅₀ value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC₅₀ value of 79 nM.

HY-114368

Kira8	Inhibitor	98.90%
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC₅₀ of 5.9 nM.

HY-17537

APY29	Inhibitor	99.90%
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC₅₀ of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.

HY-U00459

GSK2850163	Inhibitor	98.52%
GSK2850163 is a novel 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.

HY-19710

MKC3946	Inhibitor	99.21%
MKC3946 is a potent IRE1α inhibitor, used for cancer research.

HY-W018161

Hexadecanedioic acid	Inhibitor	98.0%
Hexadecanedioic acid (Thapsic acid) is an orally active metabolite produced by B. uniformis. Hexadecanedioic acid inhibits IRE1α-XBP1s-mediated flipogenesis and ferroptosis. Hexadecanedioic acid downregulates XBP1 and Hrd1 expression, activates the Nrf2/SLC7A11/GPX4 pathway. Hexadecanedioic acid can be used for the research of metabolic-associated fatty liver disease.

HY-107400

B I09	Inhibitor	99.35%
B I09 is an IRE-1 RNase inhibitor, with an IC₅₀ of 1230 nM.

HY-139212

IXA6	Activator	99.29%
IXA6 is a novel IRE1/XBP1s activator, and can induce IRE1 RNase activity.

HY-W014605

Diphenylcyclopropenone	Activator	99.88%
Diphenylcyclopropenone (Diphencyprone) is a potent hapten acting as a topical immunomodulatory agent, which induces an allergic contact dermatitis. Diphenylcyclopropenone induces an increase of cell-surface thiols in cells of a human monocytic cell line, THP-1. Diphenylcyclopropenone acts on the autoreactive T-lymphocytes within the follicular milieu to induce Apoptosis. Diphenylcyclopropenone can be used for alopecia areata research.

HY-136735

IRE1α kinase-IN-1	Inhibitor	98.94%
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC₅₀ of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC₅₀=80 nM).

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IRE1

IRE1

IRE1 Related Products (71)

Recombinant Proteins (2)

Antibodies (2)

IRE1 Related Products (71):