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-19696B

Tauroursodeoxycholate dihydrate	Inhibitor	99.96%
Tauroursodeoxycholate dehydrate is an orally active taurine conjugate of Ursodeoxycholic acid (HY-13771). Tauroursodeoxycholate dehydrate inhibits caspase-3/7, Apoptosis, IRE1α/TRAF2/NF-κB, prevents JNK phosphorylation, inhibits ROS generation, and activates Akt signaling. Tauroursodeoxycholate dehydrate prevents cataract formation, reduces renal tubular damage in type 2 diabetic mice, reduces I/R injury in liver, and inhibits intestinal inflammation and barrier disruption in nonalcoholic fatty liver disease.

HY-W020952

Palladium(Ⅱ) acetylacetonate	Activator	98.2%
Palladium(II) acetylacetonate is a metal-organic complex. Palladium(II) acetylacetonate upregulates the expression of GRP78, ATF-4, XBP-1, CHOP, and phosphorylated c-Jun. Palladium(II) acetylacetonate induces Apoptosis. Palladium(II) acetylacetonate has anticancer effects against non-small cell lung cancer, gastric cancer, leukemia, and cervical cancer.

HY-161672

G-5758	Inhibitor	98.91%
G-5758 is a selective and orally effective IRE1α inhibitor with an IC₅₀ of 38 nM (detected by the XBP1s luciferase reporter cell assay). G-5758 is still well tolerated in rats at oral doses up to 500 mg/kg. G-5758 can be used in the research of multiple myeloma.

HY-176040

IXA62	Inhibitor	99.55%
IXA62 is an orally active and selective IRE1/XBP1s activator (EC₅₀ = 0.31 μM) that reduces Aβ secretion. IXA62 enhances glucose-stimulated insulin secretion from rat insulinoma cells.

HY-N3000

6-Methoxydihydrosanguinarine	Activator	99.88%
6-Methoxydihydrosanguinarine is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer.

HY-U00460

3,6-DMAD hydrochloride	Inhibitor	99.50%
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.

HY-124646

KIRA-7	Inhibitor	99.09%
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.

HY-12399

MKC9989	Inhibitor	98.33%
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC₅₀ of 0.23 to 44 μM.

HY-18509

IRE1α kinase-IN-2	Inhibitor	99.24%
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.

HY-153773

Z4P	Inhibitor	98.29%
Z4P is a BBB-penetrable IRE1 inhibitor with an IC₅₀ of 1.13 μM. Z4P in combination with Temozolomide (HY-17364) inhibits the growth and recurrence of glioblastoma and has anti-tumor activity.

HY-155068

FC-116	Inhibitor	98.04%
FC-11 is a tubulin inhibitor. FC-116 inhibits the proliferation of colorectal cancer (CRC) cells, with IC₅₀ values of 4.52 nM for HCT116 cells and 18.69 nM for CT26 cells. FC-11 can induce ER stress to generate excess ROS, leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-116 exerts potent anti-tumor effects in vivo. FC-11 can be used for the study of colorectal cancer.

HY-107371

6-Bromo-2-hydroxy-3-methoxybenzaldehyde	Inhibitor	99.96%
6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) (Compound 3-5) is a selective and potent IRE-1α inhibitor with an IC₅₀ value of 0.08 μM. 6-Bromo-2-hydroxy-3-methoxybenzaldehyde can be used for research on diseases associated with the unfolded protein response (UPR), such as cancer and autoimmune diseases.

HY-10255AS

Sunitinib-d₁₀	Inhibitor	99.89%
Sunitinib-d₁₀ (SU 11248-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. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.

HY-178946

IA107	Inhibitor	98.14%
IA107 is a potent, selective, and allosteric IRE1α RNase (IC₅₀ = 16 nM (non phosphorylated), IC₅₀ = 9 nM (phosphorylated)) inhibitor. IA107 can inhibit endoplasmic reticulum stress-induced XBP1 mRNA splicing and protein expression, and has no cytotoxicity.

HY-10255R

Sunitinib Malate (Standard)	Inhibitor
Sunitinib (Malate) (Standard) is the analytical standard of Sunitinib (Malate). This product is intended for research and analytical applications. 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. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.

HY-U00459B

GSK2850163 hydrochloride	Inhibitor
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-114368A

Kira8 Hydrochloride	Inhibitor	98.03%
Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC₅₀ of 5.9 nM.

HY-142659

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

HY-158393

IRE1a-IN-2	Inhibitor
IRE1a-IN-2 (Compound 30) is an IRE1α inhibitor, with an IC₅₀ of over than 200 nM for XBP1 mRNA. IRE1a-IN-2 can be used for the research of cancer.

HY-158386

IRE1a-IN-1	Inhibitor
IRE1a-IN-1 (Compound 10) is an IRE1α inhibitor, with an IC₅₀ of less than 100 nM for XBP1 mRNA. IRE1a-IN-1 can be used for the research of cancer.

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IRE1

IRE1

IRE1 Related Products (71)

Recombinant Proteins (2)

Antibodies (2)

IRE1 Related Products (71):