NXT629 (NXT-629) is a potent, selective PPARα antagonist with IC50 of 77 nM (human PPARα), no effect against PPARδ and PPARγ (IC50>30 uM).
NXT629 inhibited agonist-induced transcription of PPARα-regulated genes, demonstrating target engagement in chronic lymphocytic leukemia (CLL) cells.
NXT629 induced apoptosis of CLL cells even in the presence of a protective microenvironment.
NXT629 reduces the number of chronic leukemia cells undergoing cell division with IC50 of 9.6 uM.
NXT629 reduces CLL tumor burden delays disease progression of CLL in CLL mouse model.
