Cayman Mutant Idh1-In-1; Purity- Greater Than Or Equal To 98%; Si

Mutant IDH1-IN-1 is a selective inhibitor of the cancer-associated enzyme mutant isocitrate dehydrogenase 1 (IDH1; Item No. ) with IC₅₀ values of 42, 4, and 80 nM for homozygous R132H and R132C mutant and heterozygous R132H wild-type enzymes, respectively, for converting α-ketoglutarate (α-KG) to 2-hydroxyglutaric acid (2-HG). It is selective for IDH1 mutant conversion of α-KG to 2-HG over homozygous wild-type enzyme conversion of isocitrate to α-KG (IC₅₀ = 1,998 nM) and over IDH2 (IC₅₀s = >10,000 nM). Mutant IDH1-IN-1 inhibits 2-HG production in vitro (IC₅₀ = 81.5 nM in HEK293 cells expressing IDH1^R132H). It allosterically binds to mutant IDH1 in a magnesium-dependent manner.

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