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抑制剂描述: 产品名称:YU238259 产品别名:见爱必信官网 英文别名:YU238259 靶点:HDR CAS:1943733-16-1 纯度:98% 外观:见爱必信官网 保存方法:-20℃ 描述: YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays. 溶解性:DMSO :84 mg/mL (182.6 mM) 体外研究: YU238259 is an inhibitor of homology-dependent DNA repair, with no effect on PARP activity. YU238259 shows cytotoxicity in BRCA2-deficient cells, with a low LD50 of 8.5 μM. YU238259 (0-5 μM) causes a potent, dose-dependent decrease in HDR efficiency in U2OS DR-GFP or U2OS EJ5-GFP cells, but with no effect on NHEJ frequency. YU238259 (0-10 μM) exhibits synthetic lethality with loss of frequently mutated tumor suppressors, and shows synergism with radiotherapy (IR) and DNA-damaging chemotherapy that is potentiated by BRCA2 loss. 体内研究:YU238259 (3 mg/kg, i.p.) inhibits the growth of BRCA2-deficient tumor xenografts in nude mice.
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