D-I03 是一种选择性 RAD52 抑制剂，Kd 为 25.8 µM。D-I03 抑制 RAD52 依赖性单链退火 (SSA) 和 D 环形成，IC50 分别为 5 µM 和 8 µM。D-I03 抑制 BRCA1 和 BRCA2 缺陷细胞的生长，并抑制顺铂诱导的 RAD52 病灶形成，但对 RAD51 无影响。
货号:ajcx16076
CAS:688342-78-1
分子式:C23H36N6S
分子量：428.64
溶解度:DMSO: ≥ 100 mg/mL (233.30 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 µM and 8 µM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin[1][2].

[1]. Huang F, et al. Targeting BRCA1- and BRCA2-deficient cells with RAD52 small molecule inhibitors. Nucleic Acids Res. 2016 May 19;44(9):4189-99. [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. [3]. Sullivan-Reed K, et al. Simultaneous Targeting of PARP1 and RAD52 Triggers Dual Synthetic Lethality in BRCA-Deficient Tumor Cells. Cell Rep. 2018 Jun 12;23(11):3127-3136.