TH-287 is a potent and selective inhibitor of MTH1 (NUDT1) protein with IC50 of 0.8 nM.
TH-287 shows no relevant inhibition for MTH2,NUDT5, NUDT12,NUDT14,NUDT16 and other proteinswith known nucleoside triphosphate pyrophosphatase activity.
TH-287 causees incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts.
