AGI-5198
R132 mutant isocitrate dehydrogenase inhibitor / AGI-5198 is a potent (IC50 = 70 nM) inhibitor of mutant isocitrate dehydrogenase 1(IDH1).1 It is selective for the R132H-IDH1 mutant and does not affect wild type cells.2 This mutation results in loss-of-function for oxidative decarboxylation of isocitrate and gain-of-function for production of the oncometabolite R-2-hydroxyglutarate (R-2HG) form alpha-ketoglutarate (2-OG).
Biochemicals & reagents
1355326-35-0
1) Popovici-Muller et al. (2012), Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG In Vivo; ACS Med.Chem.Lett. 3 850 2) Rohle et al. (2013), An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells; Science 340 626
-20°C
TARGET: Dehydrogenase (GAPDH, GPDH, IMPDH, PHGDH, LDH, DHODH, ALDH, GDH, IDH, UGDH, DPD, DHPDH, KGDH, PDH, and MDH); Energy production -- PATHWAY: Mitochondrial function; NAD, NADP pathways -- DISEASE AREA: Cancer