TH588
MTH1/NUDT1 inhibitor / TH588 is a first-in-class nudix hydrolase family inhibitor.1 MTH1/NUDT1 is a family member that “sanitizes” oxidized deoxynucleotide triphosphates (dNTP) preventing their incorporation into DNA and thus avoiding DNA damage and cell death. TH588 inhibits MTH1/NUDT1 (IC50 = 5 nM) leading to cell death in several cancer cell lines while not affecting normal cells. Active in vitro and in vivo. Recent evidence has raised doubts about the cancer-killing ability of MTH1 inhibition.2,3
Biochemicals & reagents
1609960-31-7
1) Gad et al. (2014), MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool; Nature 508 215 2) Petrocchi et al. (2016) Identification of potent and selective MTH1 inhibitors; Bioorg.Med.Chem.Lett. 26 1503 3) Kettle et al. (2016), Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival; J.Med.Chem. 59 2346
-20°C
PATHWAY: DNA damage -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer