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≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC 50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC 50 =80 nM).
In Vitro
IRE1α kinase-IN-1 (compound 31) prevents endoplasmic reticulum stress-induced IRE1α oligomerization and phosphorylation, and inhibits endoribonuclease activity in human cells. IRE1α kinase-IN-1 and is very high selectivity with >70% inhibition of only 4/455 kinases. IRE1α kinase-IN-1 inhibits recombinant G547 IRE1α KEN domain pS274 autophosphorylation with an IC 50 of 160 nM. IRE1α kinase-IN-1 inhibits tunicamycin-induced GFP-IRE1α foci in HEK293 cells with an IC 50 of 0.74 μM. IRE1α kinase-IN-1 Inhibits ATP-site LanthaScreen tracer binding to recombinant dephosphorylated G547 IRE1α KEN with an IC 50 of 0.27 μM. IRE1α kinase-IN-1 inhibits both tunicamycin- and thapsigargin-induced IRE1α-dependent splicing of XBP1 luciferase fusion mRNA in HEK293 cells with IC 50 s ranging 0.68-1.63 μM. IRE1α kinase-IN-1 (0-20 μM) inhibits IRE1α-dependent XBP1s mRNA expression in H929 cells.IRE1α kinase-IN-1 (0-20 μM) dose-dependently inhibits tunicamycin-induced expression of XBP1s in NCI-H929 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
| Peso molecular | 504.99 |
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Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Solubilidad | DMSO : 25 mg/mL (49.51 mM; ultrasonic and warming and heat to 60°C) |
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