mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 µM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma[1].
Molekulargewicht:
501.19
Formel:
C18H15Br2NO4S
Target-Kategorie:
Apoptosis,Isocitrate Dehydrogenase (IDH),PDK-1
Anwendungsbeschreibung:
MCE Product type: Reference compound
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