ire1

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).

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.

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).

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.

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.

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.

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

4μ8C (IRE1 Inhibitor III) is a highly selective and potent inhibitor of IRE1α ribonuclease (RNase) activity (IC₅₀ ≈ 6–10 μM). By forming a covalent bond with the RNase active site of IRE1α, 4μ8C specifically inhibits its ribonuclease activity, thereby blocking the splicing of XBP1 mRNA. 4μ8C can be used in research on endoplasmic reticulum stress, the unfolded protein response, immune regulation, and tumor and metabolic diseases.

STF-083010 is a selective inhibitor of the IRE1α endonuclease.

IXA4 is a highly selective, nontoxic activator of IRE1/XBP1s and reduces APP secretion by activating IRE1. IXA4-stimulated IRE1 activation also enhanced pancreatic function.

KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.

MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.

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-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.

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

IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with a Ki value of 140 nM, functioning as an ATP-competitive ligand for IRE1α [1].

IRE1α kinase-IN-7 is a chemical compound functioning as an inhibitor of IRE1α kinase, primarily utilized in the research of diseases related to endoplasmic reticulum stress.

1. Bufotalin (Bufotaline)e is a kind of poisonous secretions of toads.

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.

IRE1a-IN-2 (Compound 30), an inhibitor of IRE1α, exhibits an IC 50 exceeding 200 nM for XBP1 mRNA and is utilized in cancer research.