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编 号:F751698
分子式:C19H13BrFN5O2S
分子量:474.31
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生物活性:
UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2, a pyrimidine salvage enzyme) with an IC50 value of 16.6 μM. UCK2 can replace dihydroorotate dehydrogenase (DHODH), in a certain extent, in infected or rapidly dividing cells to continue efficient uridine salvage. UCK2 Inhibitor-3 also inhibits DNA polymerase eta and kappa with IC50s of 56 μM and 16 μM.

体外研究:
Dihydroorotate dehydrogenase (DHODH), a rate-limiting enzyme in mammalian de novo pyrimidine synthesis. UCK2 can make up for DHODH in a certain extent, in infected or rapidly dividing cells for uridine salvage. DHODH inhibition has antiviral and anticancer significance, while UCK2 Inhibitor-3 suppress nucleoside salvage in cells both in the presence and absence of DHODH inhibitors. UCK2 Inhibitor-3 (compound 135416439) is an inhibitor against pyrimidine salvage enzyme, non-competitive with Uridine and ATP with Ki values of 13 μM and 12 μM, respectively.UCK2 Inhibitor-3 (50 μM) inhibits UCK2 with inhibition rate of 31.3%.
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