TM2-115

A BIX-01294 derivative that inhibit malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death; inhibits P. falciparum 3D7 parasites in culture with IC50 of 100 nM, >22-fold more potent than IC50 toward two human cell lines and one mouse cell line; significant reduces histone H3K4me3 levels in a concentration-dependent and exposure time-dependent manner in treatment of P. falciparum parasites.

References 1. Malmquist NA, et al. Proc Natl Acad Sci U S A. 2012 Oct 9;109(41):16708-13. 2. Malmquist NA, et al. Antimicrob Agents Chemother. 2015 Feb;59(2):950-9. View Related Products by Target Histone Methyltransferase (HMTase)