2567914-01-4

TH1760 (2567914-01-4) is a potent inhibitor (IC50 = 25 nM dGTP hydrolysis; 57 nM 6-thio-dGTP hydrolysis) of the NUDIX hydrolase NUDT15, an important enzyme involved in the hydrolysis thiopurine chemotherapeutics.? It was selective against other human NUDIX proteins as well as a panel of 44 kinases and the Eurofins Cerep SafetyScreen44 panel.? It was active in AML cell lines HL-60 and NB4 as well as HCT116 3-6 colorectal carcinoma cells and 697 B-ALL cells.

TH1760 is an inhibitor of NUDIX-type 15 (NUDT15) with an IC50 value of 25 nM. TH1760 sensitizes cells to 6-thioguanine by enhancing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 enhances the anti-leukemia effect of thiopurine[1][2].

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Zhang et al. (2020), Development of a chemical probe against NUDT15; Chem. Biol. 16 1120