GSK126 is a methylindole with substituents at positions 1, 3, 4, and 6: (2S)-butan-2-yl, methyl, N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]acetamide, and 6-(piperazin-1-yl)pyridin-3-yl groups. It is a potent and highly selective inhibitor of EZH2 methyltransferase (IC50 = 9.9 nM), acting as a neuroprotective, antiatherosclerotic, antineoplastic, anti-obesity, angiogenesis inhibitor, and EC 2.1.1.43 inhibitor. It belongs to pyridines, secondary carboxamides, pyridones, N-arylpiperazines, and methylindoles.
