| Name | IRE1α kinase-IN-1 |
| Description | 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). |
| In vitro | IRE1α kinase-IN-1 (compound 31) effectively mitigates endoplasmic reticulum stress by hindering IRE1α oligomerization and phosphorylation, while also suppressing its endoribonuclease activity within human cells[1]. This compound demonstrates high specificity, showing greater than 70% inhibition for only 4 out of 455 kinases tested, indicating its select focus on IRE1α. It attenuates recombinant G547 IRE1α KEN domain pS274 autophosphorylation with an IC50 of 160 nM and disrupts ATP-site LanthaScreen tracer binding to the recombinant dephosphorylated G547 IRE1α KEN with an IC50 of 0.27 μM[1]. Additionally, it prevents tunicamycin-induced GFP-IRE1α foci formation in HEK293 cells with an IC50 of 0.74 μM and obstructs both tunicamycin- and thapsigargin-induced IRE1α-dependent XBP1 mRNA splicing, with IC50 values ranging from 0.68 to 1.63 μM in the same cell line[1]. In H929 and NCI-H929 cells, IRE1α kinase-IN-1 dose-dependently suppresses IRE1α-dependent XBP1s mRNA expression when applied at concentrations between 0 to 20 μM, demonstrating its potent inhibitory activity on tunicamycin-induced XBP1s expression[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 10 mg/mL (19.8 mM), Sonication is recommended.
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| Keywords | selectivity | reticulum | oligomerization | IRE1α kinase-IN-1 | IRE-1α kinase-IN-1 | IRE1α kinaseIN1 | IRE1α kinase IN 1 | IRE1α | IRE1alpha kinase-IN-1 | IRE1a kinase-IN-1 | IRE1 | Inositol requiring enzyme 1 | Inhibitor | inhibit | HEK293 | endoribonuclease | endoplasmic | cells | autophosphorylation |
| Inhibitors Related | B I09 | Sunitinib | 6-Bromo-2-hydroxy-3-methoxybenzaldehyde | Sunitinib Malate | D-F07 | MKC8866 | APY29 | GSK2850163 (S enantiomer) | 4μ8C | GSK2850163 | Toyocamycin | IXA4 |
| Related Compound Libraries | Bioactive Compound Library | Endoplasmic Reticulum Stress Compound Library | Kinase Inhibitor Library | Inhibitor Library | Bioactive Compounds Library Max | Fluorochemical Library | Cell Cycle Compound Library | Anti-Cancer Compound Library |
United States
