MeTC7 is a vitamin D receptor antagonist (IC50 = 2.9 µM in a fluorescence polarization assay).1 It inhibits vitamin D receptor transactivation in HEK293 cells (IC50 = 20.8 µM). It decreases the viability of OVCAR-8, OV-2008, SKOV3, Caov-3, and IGROV-1 ovarian cancer cells in a concentration-dependent manner. MeTC7 (250 nM) reduces retinoid X receptor α (RXRα) and importin-4 protein levels in OV-2008 cells. It reduces tumor growth in an SH-SY5Y neuroblastoma mouse xenograft model when administered at a dose of 10 mg/kg.
1.Khazan, N., Kim, K.K., Hansen, J.N., et al.Identification of a vitamin-D receptor antagonist, MeTC7, which inhibits the growth of xenograft and transgenic tumors in vivoJ. Med. Chem.65(8)6039-6055(2022)