IRE1 Inhibitor

IRE1 Inhibitors (54):

Cat. No.	Product Name	Effect	Purity

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.

HY-153475

IRE1α kinase-IN-9	Inhibitor
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).

HY-174991

CPD-2828	Inhibitor
CPD-2828 is an orally active and selective IRE1α inhibitor with an IC₅₀ value of 1.2 μM. CPD-2828 is promising for research of endoplasmic reticulum stress-related diseases (e.g., cancer, neurodegenerative diseases).

HY-145422

KIRA9	Inhibitor
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.

HY-145419

IRE1α kinase-IN-4	Inhibitor
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.

HY-153474

IRE1α kinase-IN-8	Inhibitor
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).

HY-123996

3-Ethoxy-5,6-dibromosalicylaldehyde	Inhibitor
3-ethoxy-5,6-dibromosalicylaldehyde is a potent, non-competitive, selective IRE1 (including IRE1α) inhibitor (IC₅₀s: ∼0.12 μM for hIRE1α-cyto; 6 μM for yeast Ire1). 3-ethoxy-5,6-dibromosalicylaldehyde inhibits XBP-1 splicing. 3-ethoxy-5,6-dibromosalicylaldehyde induces Apoptosis. 3-ethoxy-5,6-dibromosalicylaldehyde upregulates the mRNA expression level of TXNIP, while downregulating the expression level of TXN. 3-ethoxy-5,6-dibromosalicylaldehyde exhibits anticancer activity against pancreatic cancer. 3-ethoxy-5,6-dibromosalicylaldehyde significantly inhibits chikungunya virus replication.

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