D-I03 is a selective inhibitor of RAD52 with a Kd value of 25.8 µM. D-I03 inhibits ssDNA annealing via RAD52 and D-loop formation, with IC50 values of 5 µM and 8 µM, respectively.
D-I03 is a selective inhibitor of RAD52 with a Kd value of 25.8 μM.
D-I03 inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation, with IC50 values of 5 μM and 8 μM, respectively.D-I03 suppresses the growth of BRCA1- and BRCA2-deficient cells and inhibits cisplatin-induced RAD52 foci formation, but has no effect on RAD51.RAD52 (Cell-free assay) 25.8 μM(Ki)
| 动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
1.Targeting BRCA1- and BRCA2-deficient cells with RAD52 small molecule inhibitors.2016 May 19;44(9):4189-99. doi: 10.1093/nar/gkw087. Epub 2016 Feb 11.
2.Hengel SR, et al. Small-Molecule Inhibitors Targeting DNA Repair and DNA Repair Deficiency in Research and Cancer Therapy. Cell Chem Biol. 2017 Sep 21;24(9):1101-1119.
| 分子式 C23H36N6S |
分子量 428.64 |
CAS号 688342-78-1 |
储存方式 -20°C |
| 溶剂(常温) |
DMSO ≥ 100 mg/mL |
Water Insoluble |
Ethanol 10 mg/mL |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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