TH287 is a potent and selective inhibitor of MTH1 (NUDT1) protein with IC50 of 0.8 nM.
TH287 shows no relevant inhibition for MTH2,NUDT5, NUDT12,NUDT14,NUDT16 and other proteinswith known nucleoside triphosphate pyrophosphatase activity.
TH287 causees incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts.
