TH287
| CAS No. | 1609960-30-6 | Cat. No. | BCP10996 |
| Name | TH287 | ||
| Synonyms | TH-287;TH 287; | ||
| Formula | C11H10Cl2N4 | M. Wt | 269.13 |
| Description | TH287 is a potent inhibitor of human 7,8-Dihydro-8-oxoguaninetriphosphatase MTH1 (NUDT1) with an IC50 value of 5 nM and 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. TH287 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. | ||
| Pathways | Cell Cycle/DNA Damage | ||
| Targets | DNA/RNA Synthesis | ||
Structure
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