Dencatistat

Dencatistat is an inhibitor of CTP synthase 1 (CTPS1, IC50 = 0.0093 µM), the enzyme that catalyzes the rate-limiting step in the conversion of UTP to CTP. It is selective for CTPS1 over CTPS2 (IC50 = 12.62 µM). Dencatistat inhibits the proliferation of nine cell lines derived from T cell-based cancers (IC50s = 2-183 nM) and 12 cell lines derived from B cell-based cancers (IC50s = 3-356 nM). It also inhibits the proliferation of JeKo-1 mantle cell lymphoma and DoHH2 B cell lymphoma cells and induces apoptosis in MOLT-4, Jurkat, and DoHH2 cells. Dencatistat (6-50 mg/kg every other day) reduces tumor growth in a JeKo-1 mouse xenograft model.. SMILES: O=C(C1(C2=NC(NS(=O)(C3CC3)=O)=NC=C2)CCOCC1)NC(C=C4)=NC=C4C5=CN=CC(OCC)=N5. InChi Code: InChI=1S/C24H27N7O5S/c1-2-36-21-15-25-14-18(28-21)16-3-6-20(27-13-16)30-22(32)24(8-11-35-12-9-24)19-7-10-26-23(29-19)31-37(33,34)17-4-5-17/h3,6-7,10,13-15,17H,2,4-5,8-9,11-12H2,1H3,(H,26,29,31)(H,27,30,32). InChi Key: WVCJRTCHVUNXST-UHFFFAOYSA-N