GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic ( IC 50 of 1.8 nM) and cellular assays ( IC 50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC 50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells). GCN2-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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