Mutant IDH1-IN-7 is a highly selective inhibitor of Isocitrate Dehydrogenase 1 (IDH1) with R132H mutation (IC50 = 0.26 µM, Kd = 2.1 µM) and R132C mutation (IC50 = 1.1 µM). It does not inhibit wild-type IDH1, IDH2-wt, or IDH2R140Q. Moreover, Mutant IDH1-IN-7 reduces the production of 2-hydroxyglutarate (2-HG) in U87-MG R132H cells (EC50 = 0.55 µM) and exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells.
Target-Kategorie:
Isocitrate Dehydrogenase (IDH)
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