TH588 HCl (TH-588; TH 588), the hydrochloride salt of TH-588, is a potent
inhibitor of human 7,8-Dihydro-8-oxoguaninetriphosphatase MTH1 (NUDT1) with anti-cancer activity. It inhibits MTH1 with an IC50 of 5 nM and has good metabolic stability. Cancers have
dysfunctional redox regulation resulting in reactive oxygen species
production, damaging both DNA and free dNTPs. The MTH1 protein sanitizes
oxidized dNTP pools to prevent incorporation of damaged bases during
DNA replication. TH588 a first-in-class nudix hydrolase family inhibitor
that potently and selectively engages and inhibits the MTH1 protein in
cells. Protein co-crystal structures demonstrate that the inhibitor
binds in the active site of MTH1.
纯度:≥98%
CAS:1640282-30-9