GSK2850163 |
| Katalog-Nr.GC32857 |
GSK2850163 ist ein neuartiger Inhibitor des Inositol-erfordernden Enzyms 1 alpha (IRE1α), das die IRE1α-KinaseaktivitÄt und RNase-AktivitÄt mit IC50-Werten von 20 bzw. 200 nM hemmen kann.
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Cas No.: 2121989-91-9
Sample solution is provided at 25 µL, 10mM.
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GSK2850163 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.
GSK2850163 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 could be reduced in a dose-dependent manner by GSK2850163. Increasing concentrations of GSK2850163 are capable of reducing the increased XBP 1 transcriptional activity. Two additional kinases are weakly inhibited by GSK2850163: Ron (IC50=4.4 μM) and FGFR1 V561M (IC50=17 μM)[1].
[1]. Nestor O. Concha, et al. Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity. Molecular Pharmacology December 2015, 88 (6) 1011-1023.
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