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Isocitrate dehydrogenase (IDH) inhibitors target the mutant IDH1 and IDH2 enzymes found in several cancers. The normal enzymes convert isocitrate to α-ketoglutarate, but recurrent mutations at IDH1 R132 or IDH2 R140 and R172 change their activity. In 2009 IDH1 and IDH2 mutations were reported in a large share of gliomas, and mutant IDH1 was shown to produce 2-hydroxyglutarate. This metabolite inhibits α-ketoglutarate-dependent enzymes and alters DNA and histone methylation. AGI-5198 inhibits mutant IDH1 and AGI-6780 mutant IDH2, and both were reported in 2013 to promote differentiation of tumor cells. Enasidenib targets mutant IDH2, while vorasidenib, IDH-305 and BAY-1436032 act on mutant IDH1.
IDH1 ligand 1 serves as a negative control for isocitrate dehydrogenase 1 (IDH1). It exhibits no measurable affinity for wild-type IDH1, with an IC50 greater than 10,000 nM. This compound is useful in differentiating specific IDH1 interactions in research applications, allowing for the assessment of ligand-target relationships in biochemical assays.
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