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BRD2879 is a potent and cell-active inhibitor of IDH1-R132H with a markedly different structure from previously reported probes with (IC50 = 50 nM for inhibiting IDH1-R132H enzyme). BRD2879 represents a new structural class of mutant IDH1 inhibitors that, with optimization, may prove useful in the study of this enzyme and its role in cancer.

BRD2879 is a potent IDH1-R132H inhibitor with IC50 values of 0.05, 2.5, >20, >20 μM for IDH1-R132H, IDH1-R132C, IDH1-WT, IDH2-R140Q, respectively. BRD2879 reduces (R)-2-hydroxyglutarate (R-2HG) levels[1].

R132H IDH1: 0.05 μM (IC₅₀); R132C IDH1: 2.5 μM (IC₅₀); IDH1 wt: >20 μM (IC₅₀); IDH2-R140Q: >20 μM (IC₅₀)

[1] Law JM, et al. Discovery of 8-Membered Ring Sulfonamides as Inhibitors of Oncogenic Mutant Isocitrate Dehydrogenase 1. ACS Med Chem Lett. 2016 Aug 18;7(10):944-949. DOI:10.1021/acsmedchemlett.6b00264