mth1/nudt1

BAY-707, a highly potent and selective substrate-competitive inhibitor of MTH1 (NUDT1) with an IC50 of 2.3 nM, is well-tolerated in mice and exhibits a favorable pharmacokinetic (PK) profile compared to other MTH1 compounds. However, it demonstrates a clear lack of anticancer efficacy both in vitro and in vivo[1].

TH287 is a potent inhibitor of MTH1 (NUDT1), less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.

TH588 hydrochloride, a first-in-class inhibitor of the nudix hydrolase family, selectively and effectively binds to and inhibits MTH1 with an IC50 value of 5 nM.

(S)-crizotinib (ent-crizotinib) （IC50 of 72 nM）, an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.