TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) with an IC50 value of 0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.IC50 value: 0.8 nM [1]Target: MTH1 inhibitorTH287 is considered a new target for cancer therapy. TH287 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family. TH287 has been shown to selectively kill a variety of cancer cell lines, but is rapidly metablized, so not as useful for in vivo studies.
[1]. Gad H, et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature. 2014 Apr 10;508(7495):215-21.