GSK2850163 (hydrochloride)
CAS No. : 2319838-09-8
(Synonyms: GSK163 (hydrochloride))
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| Cat. No. : | HY-U00459B |
| M.Wt: | 482.87 |
| Formula: | C24H30Cl3N3O |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively. IC50 & Target:IC50: 20 nM (IRE1α kinase activity), 200 nM (IRE1α RNase activity)[1] In Vitro: GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively. The increased autophosphorylation of IRE1α can be reduced in a dose-dependent manner by GSK2850163 hydrochloride. Increasing concentrations of GSK2850163 hydrochloride are capable of reducing the increased XBP 1 transcriptional activity. Two additional kinases are weakly inhibited by GSK2850163 hydrochloride: Ron (IC50=4.4 μM) and FGFR1 V561M (IC50=17 μM)[1].
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