YK-11 is an androgen receptor partial agonist that activates androgen receptor transcriptional activity in HEK293 cells overexpressing androgen receptors when used at a concentration of 0.1 μM.1 It induces expression of the androgen receptor target genes FKBP51 and FGF18 in HEK293 cells when used at a concentration of 10 μM. YK-11 accelerates nuclear translocation of androgen receptors without inducing interaction between the androgen receptor N- and C-termini. In C2C12 cells, YK-11 (500 nM) increases expression of the myogenic regulatory factors MyoD, Myf5, and myogenin, as well as follistatin (Fst), and induces myogenic differentiation.2 YK-11 also accelerates proliferation and mineralization and increases expression of the osteoblast differentiation markers osteoprotegerin and osteocalcin in MC3T3-E1 mouse osteoblast cells.3
1.Kanno, Y., Hikosaka, R., Zhang, S.-Y., et al.(17α,20E)-17,20-[(1-Methoxyethylidene)bis(oxy)]-3-oxo-19-norpregna-4,20-diene-21-carboxylic acid methyl ester (YK11) is a partial agonist of the androgen receptorBiol. Pharm. Bull.34(3)318-323(2011) 2.Kanno, Y., Ota, R., Someya, K., et al.Selective androgen receptor modulator, YK11, regulates myogenic differentiation of C2C12 myoblasts by follistatin expressionBiol. Pharm. Bull.36(9)1460-1465(2013) 3.Yatsu, T., Kusakabe, T., Kato, K., et al.Selective androgen receptor modulator, YK11, up-regulates osteoblastic proliferation and differentiation in MC3T3-E1 cellsBiol. Pharm. Bull.41(3)394-398(2018)