化合物IRE1α kinase-IN-1 T9564

Product Introduction
Bioactivity


英文名: IRE1α kinase-IN-1

描述: IRE1α kinase-IN-1 是IRE1α 的选择性抑制剂(IC50为 77 nM)，对 IRE1α 的选择性高于 IRE1β 亚型 100 倍。它抑制内质网诱导的 IRE1α 寡聚和自磷酸化，并抑制 IRE1α RNase 活性 (IC50=80 nM)。

体外活性: IRE1α kinase-IN-1 (compound 31) prevents endoplasmic reticulum stress-induced IRE1α oligomerization and phosphorylation, and inhibits endoribonuclease activity in human cells[1].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 IC50 of 160 nM. IRE1α kinase-IN-1 inhibits tunicamycin-induced GFP-IRE1α foci in HEK293 cells with an IC50 of 0.74 μM. IRE1α kinase-IN-1 Inhibits ATP-site LanthaScreen tracer binding to recombinant dephosphorylated G547 IRE1α KEN with an IC50 of 0.27 μM[1].IRE1α kinase-IN-1 inhibits both tunicamycin- and thapsigargin-induced IRE1α-dependent splicing of XBP1 luciferase fusion mRNA in HEK293 cells with IC50s ranging 0.68-1.63 μM[1].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[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 10 mg/mL (19.8 mM)


关键字: endoribonuclease | Inositol requiring enzyme 1 | cells | IRE1a kinase-IN-1 | IRE1 | oligomerization | IRE-1α kinase-IN-1 | selectivity | IRE1α kinase IN 1 | Inhibitor | IRE1α kinase-IN-1 | inhibit | IRE1alpha kinase-IN-1 | HEK293 | autophosphorylation | reticulum | IRE1α kinaseIN1 | endoplasmic

相关产品: STF-083010 | B I09 | APY29 | IRE1α kinase-IN-9 | MKC3946 | GSK2850163 (S enantiomer) | IXA4 | 6-Bromo-2-hydroxy-3-methoxybenzaldehyde | MKC8866 | KIRA6

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Endoplasmic Reticulum Stress Compound Library | Kinase Inhibitor Library | Inhibitor Library | ER stress pathway inhibitor/inducer kit | Bioactive Compound Library

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