D-I03 |
رقم الكتالوجGC39149 |
D-I03 هو مثبط انتقائي لـ RAD52 بقدرة 25.8 ميكرومترD-I03 يمنع على وجه التحديد التلدين الفردي المعتمد على RAD52 (SSA) وتشكيل الحلقة D مع IC50s من 5 ميكرومتر و 8 ميكرومتر ، على التواليD-I03 يثبط نمو الخلايا التي تعاني من نقص BRCA1 و BRCA2 ويمنع تكوين بؤر RAD52 التي يسببها التلف ، ولكنه لا يؤثر على بؤر RAD51 التي يسببها سيسبلاتين
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Cas No.: 688342-78-1
Sample solution is provided at 25 µL, 10mM.
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.
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