IRE1 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.

1ACTA is an IRE1α S-Nitrosylation inhibtor, maintaining the endoplasmic reticulum stress response under nitrosative stress.

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.

IRE1-IN-2 (compound G15) is a potent IRE1 inhibitor. IRE1-IN-2 inhibits FFA-induced lipid accumulation with an IC₅₀ of 2.06 μM.

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.

DL-Aspartic acid (Standard) is the analytical standard of DL-Aspartic acid. This product is intended for research and analytical applications. DL-Aspartic acid (DL-Asp-OH) is a kind of biological materials or organic compounds that are widely used in life science research.

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.

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.

D-F07 is a prodrug with an aldehyde shielding group and an IRE-1 inhibitor that induces Apoptosis. D-F07 has antitumor activity.

Lard oil is an orally active biochemical reagent. Lard oil upregulates PERK, eIF2a, CHOP, OPN, TLR2, TLR4, TNF-α, and downregulates GRP78 and IRE1a. Lard oil induces responses such as body fat accumulation, elevated serum insulin levels, increased HOMA-IR, hepatic ectopic lipid deposition, hepatic endoplasmic reticulum stress, and hepatic inflammation. Lard oil can be used in studies related to diet-induced obesity, insulin resistance, and non-alcoholic fatty liver disease.

IRE1α kinase-IN-10 (GP29) is an IRE1α kinase inhibitor. IRE1α kinase-IN-10 can be used for the research of endoplasmic reticulum stress-related diseases.

6-Bromo-2-hydroxy-3-methoxybenzaldehyde (Standard) (NSC95682 (Standard)) is the analytical standard of 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (HY-107371). This product is intended for research and analytical applications. 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.

B I09 (Standard) is the analytical standard of B I09 (HY-107400). This product is intended for research and analytical applications. B I09 is an IRE-1 RNase inhibitor, with an IC₅₀ of 1230 nM.

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. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.

MKC8866 (Standard) is the analytical standard of MKC8866 (HY-104040). This product is intended for research and analytical applications. 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.