ire-1

D-F07 is a novel fluorescent IRE-1 RNase inhibitor and a tricyclic chromone with potential anticancer activity.

B I09, an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells.

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α), effectively inhibiting both its RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).

3,6-DMAD dihydrochloride is an acridine derivative and a potent inhibitor of the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride can induce IL-6 secretion by exploiting the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride is a potent inhibitor of the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride has inhibitory effects on IRE1α oligomerization and RNase activity. 3,6-DMAD dihydrochloride can be used in cancer research.

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

Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.

6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC-95682) is an inhibitor of IRE-1α with an IC50 value of 0.08 μM.

IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, is a potent inhibitor of IRE-1α used in research on diseases related to the unfolded protein response and regulated IRE1-dependent decay (RIDD) [1].

IRE1α kinase-IN-9 (compound 2) is a potent inhibitor of IRE-1α with an average IC50 value of less than 0.1 μM, and it is suitable for research into diseases related to the unfolded protein response or regulated IRE1-dependent decay (RIDD) [1].

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM, displaying 100-fold selectivity over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, as well as IRE1α RNase activity (IC50=80 nM).

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

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

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

Sunitinib D10 is a deuterium labeled Sunitinib. Sunitinib is a inhibitor of multi-targeted receptor tyrosine kinase(IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively).

MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro). MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibit prostate cancer (PCa) tumor growth.

KIRA-7 is an imidazopyrazine compound. KIRA-7 has an anti-fibrotic effect. KIRA-7 binds the IRE1α kinase (IC50: 110 nM) to allosterically inhibit its RNase activity.

Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycetes, functioning as an XBP1 inhibitor and inhibiting IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM), and induces apoptosis.

1ACTA (IRE1αS-nitrosylation inhibitor) is a compound that helps maintain the endoplasmic reticulum stress response under conditions of nitrosative stress.

Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. It significantly promotes Nur77 expression and apoptosis, exhibiting excellent growth inhibitory effects on HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, leading to apoptosis. This compound is applicable in cancer research.

IRE1-IN-2 (compound G15) functions as a potent inhibitor of IRE1. It effectively suppresses lipid accumulation induced by FFA, exhibiting an IC50 value of 2.06 μM.

CPD-2828 is an orally active selective inhibitor of IRE1α, with an IC50 value of 1.2 μM. It shows potential for research into endoplasmic reticulum stress-related diseases, such as cancer and neurodegenerative disorders.

APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.

IRE1α kinase-IN-2 is a highly potent inhibitor of IRE1α kinase, demonstrating an EC50 of 0.82 μM and impeding IRE1α kinase autophosphorylation with an IC50 of 3.12 μM. It also effectively inhibits the splicing of XBP1 mRNA in wild-type cell lines.