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Methyl gerfelin inhibits osteoclast differentiation by binding 3 major cellular proteins: glyoxalase 1 (GLO1), sterol binding protein 2 (SCP2), and small glutamine-rich tetratricopeptide repeat containing protein A (SGTA). Methyl gerfelin is a potent GLO1 inhibitor related to the flavonoid class[1][2].

[1] Kanoh N, et al. Dual structure-activity relationship of osteoclastogenesis inhibitor methyl gerfelin based on TEG scanning. Bioconjug Chem. 2013 Jan 16;24(1):44-52. DOI:10.1021/bc3003666
[2] Perez C, et al. Metal-Binding Pharmacophore Library Yields the Discovery of a Glyoxalase 1 Inhibitor. J Med Chem. 2019 Feb 14;62(3):1609-1625. DOI:10.1021/acs.jmedchem.8b01868