TM2-115 is a BIX-01294 derivative that inhibit malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death.
TM2-115 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.
TM2-115 significant reduces histone H3K4me3 levels in a concentration-dependent and exposure time-dependent manner in treatment of P. falciparum parasites.
