IDH1 Inhibitor 5

IDH1 Inhibitor 5 (compound 2) is an IDH1 (isocitrate dehydrogenase 1) inhibitor. IDH1 Inhibitor 5 inhibits MOG cells and wild-type IDH1 glioma cells with expressing exogenous mutant IDH1 R132H protein with IC50s of 64.4 and 34.9 nM, respectively[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Isocitrate Dehydrogenase (IDH)

IC50: 64.4 nM (MOG cells), 34.9 nM (wild-type IDH1 glioma cells with expressing exogenous mutant IDH1 R132H protein)[1]

IDH1 Inhibitor 5 (0-10 μM; 1 h) shows cellular potency in MOG cells[1]. Cell Cytotoxicity Assay[1] Cell Line: MOG cell line and wild-type IDH1 glioma cells with expressing exogenous mutant IDH1 R132H protein Concentration: 0-10 μM Incubation Time: 1 hour Result: Showed cellular potency to MOG cells and wild-type IDH1 glioma cells with expressing exogenous mutant IDH1 R132H protein with IC50s of 64.4 and 34.9 nM, respectively.

[1]. Huang C, et al. Diminishing GSH-Adduct Formation of Tricyclic Diazepine-based Mutant IDH1 Inhibitors. ACS Med Chem Lett. 2022 Mar 28;13(4):734-741.