NXT629 is a selective and highly efficient PPAR-α antagonist with anticancer activity. It inhibits PPARδ, PPARγ, Erβ, GR, and TRβ and can be used in research on ovarian cancer and melanoma.

PPARα (human):77 nM, PPARγ (human):15 μM, ERβ:15.2 μM, PPARδ (human):6 μM, GR:32.5 μM

NXT629 (compound 33) is a potent and selective PPAR-α antagonist with an IC50 of 77 nM for human PPARα, as well as weaker effects on other nuclear hormone receptors (e.g., PPARδ, PPARγ, Erβ, GR, and TRβ) with IC50s of 6.0 μM, 15 μM, 15.2 μM, 32.5 μM, and >100 μM, respectively.[1]
The competitive inhibitory ability of NXT629 on PPARα, PPARβ/δ and PPARγ was also validated, with corresponding IC50s of 2.3 μM, 35.1 μM and 6.9 μM, respectively.[2]

NXT629 exhibits low oral bioavailability in mice and rats. NXT629 administered intraperitoneally (30 mg/kg once daily for 6 weeks) significantly slowed down the growth of subcutaneous SKOV-3 tumors in nude mice and showed inhibition of subcutaneous B16F10 tumor growth in C57Bl/6 mice. In addition, NXT629 (30 mg/kg, intraperitoneal injection) showed weak anti-angiogenic activity in FGF-induced angiogenesis. NXT629 (3 and 30 mg/kg, intraperitoneal injection) also reduced experimental metastasis of B16F10 melanoma cells in the lungs of mice. [2]