IRE1

By Targets:	IRE1 (35) Antibiotic (1) Apoptosis (6) Autophagy (3) CDK (1) Fungal (1) Isotope-Labeled Compounds (1) Mitophagy (3) PDGFR (3) Reactive Oxygen Species (1) VEGFR (3)
By Research Areas:	Cancer (23) Infection (1) Inflammation/Immunology (4) Metabolic Disease (2) Neurological Disease (2)

Targets Recommended: IRE1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19707

4μ8C

30+ Cited Publications

IRE1 Inhibitor III
IRE1 Metabolic Disease

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

4μ8C 30+ Cited Publications IRE1 Inhibitor III	IRE1	Metabolic Disease
4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of *IRE1α*.

HY-136735

IRE1α kinase-IN-1	IRE1	Neurological Disease Cancer
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) ^[1].

HY-153474

IRE1α kinase-IN-8	IRE1	Others
IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, is a potent *IRE-1α* inhibitor. IRE1α kinase-IN-8 can be used for research in diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) ^[1].

HY-153475

IRE1α kinase-IN-9	IRE1	Cancer
IRE1α kinase-IN-9 (compound 2) is a potent IRE-1α inhibitor，exhibits an average IC₅₀ value of <0.1 μM. IRE1α kinase-IN-9 can be used for research in diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) ^[1].

HY-145418

IRE1α kinase-IN-3

IRE1 Others

IRE1α kinase-IN-3 (compound 2) is a potent IRE1α inhibitor with an K_i of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α ^[1].
HY-145419

IRE1α kinase-IN-4

IRE1 Others

IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with an K_i of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α ^[1].
HY-145420

IRE1α kinase-IN-5

IRE1 Others

IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor with an K_i of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α ^[1].

IRE1α kinase-IN-3	IRE1	Others
IRE1α kinase-IN-3 (compound 2) is a potent *IRE1α* inhibitor with an K_i of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α ^[1].

IRE1α kinase-IN-4	IRE1	Others
IRE1α kinase-IN-4 (compound 6) is a potent *IRE1α* inhibitor with an K_i of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α ^[1].

IRE1α kinase-IN-5	IRE1	Others
IRE1α kinase-IN-5 (compound 7) is a potent *IRE1α* inhibitor with an K_i of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α ^[1].

HY-18509

IRE1α kinase-IN-2	IRE1	Cancer
IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC₅₀ of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC₅₀=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines ^[1].

HY-18510

IRE1α kinase-IN-7	IRE1	Others
IRE1α kinase-IN-7 (compound 4) is an IRE1α kinase inhibitor. IRE1α kinase-IN-7 can be used for research of endoplasmic reticulum stress-related diseases ^[1].

HY-142659

IRE1α kinase-IN-6

IRE1 Cancer

IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC₅₀ value of 4.4 nM.
HY-139212

IXA6

IRE1 Others

IXA6 is a novel IRE1/XBP1s activator, and can induce IRE1 RNase activity ^[1].

IRE1α kinase-IN-6	IRE1	Cancer
IRE1α kinase-IN-6 is a potent *IRE1α* inhibitor with an IC₅₀ value of 4.4 nM.

IXA6	IRE1	Others
IXA6 is a novel *IRE1/XBP1s* activator, and can induce IRE1 RNase activity ^[1].

HY-139214

IXA4 2 Publications Verification	IRE1	Neurological Disease
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 ^[1].

HY-107400

B I09

1 Publications Verification

IRE1 Cancer

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

B I09 1 Publications Verification	IRE1	Cancer
B I09 is an *IRE-1* RNase inhibitor, with an IC₅₀ of 1230 nM.

HY-145422

KIRA9	IRE1 Apoptosis	Others
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 ^[1].

HY-15845

STF-083010 30+ Cited Publications	IRE1	Cancer
STF-083010 is a specific *IRE1α* inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.

HY-104040

MKC8866 5+ Cited Publications Orin1001	IRE1	Cancer
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 ^[1]. 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-153773

Z4P	IRE1	Cancer
Z4P is a BBB-permeable *IRE1* inhibitor (IC₅₀: 1.11 μM). Z4P inhibits Glioblastoma cell growth. Z4P prevents glioblastoma relapse when administered together with Temozolomide (HY-17364) ^[1].

HY-U00460

3,6-DMAD hydrochloride	IRE1	Cancer
3,6-DMAD hydrochloride, an acridine derivative, is a potent *IRE1α-XBP1s* pathway inhibitor. 3,6-DMAD hydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD hydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD hydrochloride can be used for research of cancer ^[1] .

HY-U00460B

3,6-DMAD dihydrochloride	IRE1	Cancer
3,6-DMAD dihydrochloride, an acridine derivative, is a potent *IRE1α-XBP1s* pathway inhibitor. 3,6-DMAD dihydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD dihydrochloride can be used for research of cancer ^[1] .

HY-145425

PAIR2	IRE1	Cancer
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 ^[1].

HY-17537

APY29 5+ Cited Publications	IRE1	Cancer
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 ^[1].

HY-114368A

Kira8 Hydrochloride AMG-18 Hydrochloride	IRE1	Inflammation/Immunology
Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective *IRE1α* inhibitor that allosterically attenuates IRE1α RNase activity with an IC₅₀ of 5.9 nM ^[1].

HY-114368

Kira8 5+ Cited Publications AMG-18	IRE1	Inflammation/Immunology
Kira8 (AMG-18) is a mono-selective *IRE1α* inhibitor that allosterically attenuates IRE1α RNase activity with an IC₅₀ of 5.9 nM ^[1].

HY-U00459

GSK2850163 3 Publications Verification	IRE1	Cancer
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-U00459B

GSK2850163 hydrochloride	IRE1	Cancer
GSK2850163 hydrochloride 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-103248

Toyocamycin 4 Publications Verification Vengicide	IRE1 Fungal Antibiotic Apoptosis CDK	Infection Cancer
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 ^[1] .

HY-19710

MKC3946

5 Publications Verification

IRE1 Cancer

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

MKC3946 5 Publications Verification	IRE1	Cancer
MKC3946 is a potent *IRE1α* inhibitor, used for cancer research.

HY-107371

6-Bromo-2-hydroxy-3-methoxybenzaldehyde NSC95682	IRE1	Cancer
6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an *IRE-1α* inhibitor with an IC₅₀ of 0.08 μM, extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5.

HY-12399

MKC9989

IRE1 Cancer

MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC₅₀ of 0.23 to 44 μM.
HY-U00459A

GSK2850163 (S enantiomer)

IRE1 Others

GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. GSK2850163 is an inositol-requiring enzyme-1 alpha (IRE1a) inhibitor.

MKC9989	IRE1	Cancer
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits *IRE1α* with an IC₅₀ of 0.23 to 44 μM.

GSK2850163 (S enantiomer)	IRE1	Others
GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. GSK2850163 is an inositol-requiring enzyme-1 alpha (IRE1a) inhibitor.

HY-19708

KIRA6 10+ Cited Publications	IRE1	Metabolic Disease Inflammation/Immunology Cancer
KIRA6 is an advanced small-molecule *IRE1α* RNase kinase inhibitor with an IC₅₀ of 0.6 µM . KIRA6 can trigger an apoptotic response ^[1].

HY-124646

KIRA-7	IRE1	Inflammation/Immunology
KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC₅₀ of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect ^[1].

HY-N0878

Bufotalin 4 Publications Verification	Apoptosis Reactive Oxygen Species	Cancer
Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation ^[1] .

HY-10255A

Sunitinib Maximum Cited Publications 46 Publications Verification SU 11248	VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively ^[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of *Ire1α* by inhibiting autophosphorylation and consequent RNase activation .

HY-10255

Sunitinib Malate Maximum Cited Publications 46 Publications Verification SU 11248 Malate	PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively ^[1]. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of *Ire1α* by inhibiting autophosphorylation and consequent RNase activation .

HY-10255AS

Sunitinib-d10 SU 11248-d10
Sunitinib-d₁₀ is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

HY-10255AS1

Sunitinib-d4	Isotope-Labeled Compounds VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib-d₄ is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

Cat. No.	Product Name

HY-L054

Endoplasmic Reticulum Stress Compound Library	219 compounds
Endoplasmic reticulum (ER) contributes to the production and folding of approximately one third of cellular proteins, and is thus inextricably linked to the maintenance of cellular homeostasis and the fine balance between health and disease. However, some adverse factors negatively impact ER functions and protein synthesis, resulting in the activation of Endoplasmic reticulum stress (ER stress, ERS) and unfolded protein response (UPR) signaling pathways. The UPR is triggered when ER protein folding capacity is overwhelmed by cellular demand and the UPR initially aims to restore ER homeostasis and normal cellular functions. However, if this fails, then the UPR triggers cell death. Chronic ER stress and defects in UPR signaling are emerging as key contributors to a growing list of human diseases, including diabetes, neurodegeneration and cancer. MCE Endoplasmic Reticulum Stress Compound Library contains 219 ER stress-related compounds that mainly target PERK, IRE1, ATF6, etc. MCE ER stress library is a useful tool for researching ER stress and related diseases.

Endoplasmic Reticulum Stress Compound Library

219 compounds

Endoplasmic reticulum (ER) contributes to the production and folding of approximately one third of cellular proteins, and is thus inextricably linked to the maintenance of cellular homeostasis and the fine balance between health and disease. However, some adverse factors negatively impact ER functions and protein synthesis, resulting in the activation of Endoplasmic reticulum stress (ER stress, ERS) and unfolded protein response (UPR) signaling pathways. The UPR is triggered when ER protein folding capacity is overwhelmed by cellular demand and the UPR initially aims to restore ER homeostasis and normal cellular functions. However, if this fails, then the UPR triggers cell death. Chronic ER stress and defects in UPR signaling are emerging as key contributors to a growing list of human diseases, including diabetes, neurodegeneration and cancer.

MCE Endoplasmic Reticulum Stress Compound Library contains 219 ER stress-related compounds that mainly target PERK, IRE1, ATF6, etc. MCE ER stress library is a useful tool for researching ER stress and related diseases.

Cat. No.	Product Name	Type

HY-162075

RF16

Fluorescent Dyes/Probes

RF16 is a fluorescent macromolecular material. RF16 precisely retains in cells to track IRE1-Halo protein with the HaloTag ligand ^[1].

RF16	Fluorescent Dyes/Probes
RF16 is a fluorescent macromolecular material. RF16 precisely retains in cells to track IRE1-Halo protein with the HaloTag ligand ^[1].

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-103248

Toyocamycin 4 Publications Verification Vengicide	Infection Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Disease Research Fields Other Antibiotics	IRE1 Fungal Antibiotic Apoptosis CDK
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 ^[1] .

HY-N0878

Bufotalin 4 Publications Verification	Classification of Application Fields Animals Source classification Disease Research Fields Steroids Cancer	Apoptosis Reactive Oxygen Species
Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation ^[1] .

Species:	Human (2)
Tag:	His (1) Tag Free (1) GST (1)
Source:	Sf9 insect cells (2)

Cat. No.	Compare	Product Name	Species	Source

HY-P73858

	IRE1 Protein, Human (sf9) Serine/threonine-protein kinase/endoribonuclease IRE1; IRE1a; ERN1; IRE1	Human	Sf9 insect cells
	IRE1 is a key serine/threonine protein kinase and endoribonuclease essential for sensing the unfolded protein response (UPR) in the endoplasmic reticulum. In cellular homeostasis, it remains monomeric by binding to HSPA5/BiP. IRE1 Protein, Human (sf9) is the recombinant human-derived IRE1 protein, expressed by Sf9 insect cells , with tag free. The total length of IRE1 Protein, Human (sf9) is 513 a.a., with molecular weight of ~65 kDa.

HY-P73256

	IRE1 Protein, Human (sf9, His-GST) Serine/threonine-protein kinase/endoribonuclease IRE1; IRE1a; ERN1; IRE1	Human	Sf9 insect cells
	IRE1 is a key serine/threonine protein kinase and endoribonuclease essential for sensing the unfolded protein response (UPR) in the endoplasmic reticulum. In cellular homeostasis, it remains monomeric by binding to HSPA5/BiP. IRE1 Protein, Human (sf9, His-GST) is the recombinant human-derived IRE1 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of IRE1 Protein, Human (sf9, His-GST) is 513 a.a., with molecular weight of ~90 kDa.

Cat. No.	Product Name	Chemical Structure

HY-10255AS1

Sunitinib-d4
Sunitinib-d₄ is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

Cat. No.	Product Name	Application	Reactivity

HY-P80828

*Phospho-IRE1* (Ser724) Antibody** ERN1; IRE1; Serine/threonine-protein kinase/endoribonuclease IRE1; Endoplasmic reticulum-to-nucleus signaling 1; Inositol-requiring protein 1; hIRE1p; IRE1-alpha; IRE1a	WB, IP	Human
Phospho-IRE1 (Ser724) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 110 kDa, targeting to Phospho-IRE1 (Ser724). It can be used for WB,IP assays with tag free, in the background of Human.


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