V-125

V-125 is an agonist of retinoid X receptors (RXRs).¹ It induces homodimerization of RXR in HCT116 cells in a two-hybrid assay (EC₅₀ = 13.8 nM). V-125 selectively induces transactivation of RXRα in human RXRα-overexpressing HCT116 cells over transactivation of RARα in human RARα-overexpressing HEK293 cells when used at concentrations of 25 and 100 nM, respectively. In vivo, V-125 (80 mg/kg in the diet) inhibits vinyl carbamate-induced lung tumor growth in mice.² Unlike the RXR agonist bexarotene , V-125 does not increase plasma triglyceride or cholesterol levels in mice.

1.Heck, M.C., C.E., W., Shahani, P.H., et al.Modeling, synthesis, and biological evaluation of potential retinoid X receptor (RXR)-selective agonists: Analogues of 4?[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene) and 6?(ethyl(5,5,8,8-tetrahydronaphthalen-2-yl)amino)nicotinic acid (NEt-TMN)J. Med. Chem.59(19)8924-8940(2016) 2.Reich, L.A., Moerland, J.A., Leal, A.S., et al.The rexinoid V?125 reduces tumor growth in preclinical models of breast and lung cancerSci. Rep.12(1)293(2022)