Selective human thymidylate kinase (hTMPK; IC50 value 1.65 µM) inhibitor that lacks inhibitory effect on the activity of purified thymidine kinase 1 (TK1). YMU1 stabilizes the conformation of ligand-induced degradation (LID) region of hTMPK and blocks the catalytic site or ATP-binding site. Blocking hTMPK by YMU1 attenuates the ATP binding-induced closed conformation that is required for phosphorylation of dTMP, and sensitizes cancer cells for low-dose doxorubicin chemotherapy.

Keywords: YMU1 | supplier | TMPK inhibtor | YMU-1 | YMU 1 | CAS [902589-96-2] | Thymidylate pathway | hTMPK | Phosphotransferase | dTTP | dTMP | doxorubicin | tuberculosis | cancer