TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19[2].IC50 & Target: IC50: 47 nM (dCTPase)In Vitro: TH1217 (compound 30) inhibits dCTPase and enhances aqueous solubility (>100 μM) and improves plasma stability in vitro(t4h=86%).
TH1217 presents suitable mouse microsomal half-lives (109 minutes).
TH1217 displays well cell permeability (8.66×10-6/1.30×10-3 cm/s) and CYP inhibition.