IRE1 Inhibitor

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

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.

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.

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.

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.

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.

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.

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.

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.

Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. 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.

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.

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

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

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.

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.

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).

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).

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.

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.

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).