TRβ antagonist NH-3 is a potent, selective antagonist of Thyroid hormone receptor beta (TRβ) with binding KD of 20 nM (hTRβ) and 93 nM (TRα1). NH-3 is TRβ-selective in both binding and inhibition of T3-induced transactivation. NH-3 blocks 1 nM T3 induced transactivation in a dose-dependent manner with IC50 of 370 nM. NH-3 inhibits PCa cell proliferation in vitro and reduced tumor size in PCa xenograft models in vivo.
