AK177 is an allosteric activator of IRE1alpha ribonuclease, with values of 480 nM and 180 nM against non-phosphorylated and phosphorylated IRE1alpha, respectively.AK177 promotes IRE1alpha-mediated cleavage of XBP1 mRNA probe in a concentration-dependent manner and binds stably to its kinase domain. However, AK177 shows poor kinase selectivity, and due to poor membrane permeability at the cellular level, it induces no significant downstream pathway activation or antiproliferative activity[1].
Molekulargewicht:
564.62
Formel:
C26H28N8O5S
Target-Kategorie:
c-Kit,IRE1,PDGFR
Anwendungsbeschreibung:
MCE Product type: Reference compound
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