Catalog No.: PC-49548Not For Human Use, Lab Use Only.
DS55980254 (DS 55980254) is potent, selective and orally active PTDSS1 (phosphatidylserine synthetase 1) inhibitor, suppresses phosphatidylserine (PS) production activity of PTDSS1 (IC50=100 nM) in cell-free assays, but not that of PTDSS2.
DS55980254 (DS 55980254) is potent, selective and orally active PTDSS1 (phosphatidylserine synthetase 1) inhibitor, suppresses phosphatidylserine (PS) production activity of PTDSS1 (IC50=100 nM) in cell-free assays, but not that of PTDSS2.
DS55980254 strongly suppressed the de novo PS synthesis in PTDSS2-KO HCT116 clone, whereas they weakly suppressed it in parental HCT116.
DS55980254 selectively suppressed the growth of PTDSS2-KO HCT116 in vitro.(
DS55980254 (10-30 mg/kg, daily, p.o.) induced tumor regression in PTDSS2-KO HCT116 and PTDSS2-KO A375 subcutaneous xenograft models, without body weight loss and severe toxicity.
DS55980254 induced selective cell death in PTDSS2-deleted cancer cells, induced ER stress downstream of PS depletion in PTDSS2-deleted tumor cells.
DS55980254 suppressed the growth of tumor containing both PTDSS2 wild-type and knockout cells in immunocompetent mice, showing potency for overcoming tumor heterogeneity by modulating the tumor immune microenvironment.
