RI-1 (415713-60-9) is a potent and selective inhibitor of RAD51 (IC50 = 5-30 μM), a highly conserved protein that catalyzes DNA repair via homologous recombination.1 It specifically reduces gene conversion in human cells and stimulates single strand annealing. It covalently binds to Cys319 on the surface of RAD51 and disrupts protein-protein interaction. It potentiates the effect of DNA-damaging agents on tumor cells and is a novel tool for studying DNA repair in cells.2 Potentiates the killing of glioblastoma cells by ionizing radiation3 and alkylating drugs4. RI-1(415713-60-9)是一种强效的选择性RAD51抑制剂(IC50 = 5-30 μM), RAD51是一种高度保守的蛋白,通过同源重组催化DNA修复 它专门减少人类细胞中的基因转换,并刺激单链退火。 它与RAD51表面的Cys319共价结合,破坏蛋白质与蛋白质的相互作用。 它增强了DNA损伤剂对肿瘤细胞的作用,是研究细胞DNA修复的新工具 通过电离辐射和烷基化药物增强对胶质母细胞瘤细胞的杀伤。
References/Citations
1) Anand et al. (2017), Rad51-mediated double-strand break repair and mismatch correction of divergent substrates; Nature, 544 377 2) Budke et al. (2012), RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells; Nucleic Acids Res., 40 7347 3) Balbous et al. (2016), A radiosensitizing effect of RAD51 inhibition in glioblastoma stem-like cells; BMC Cancer, 16 604 4) Berte et al. (2016), Targeting Homologous Recombination by Pharmacological Inhibitors Enhances the Killing response of Glioblastoma Cells Treated with Alkylating Drugs; Mol. Cancer Ther., 15 2665
CAS:
415713-60-9
Catalog Number:
10-1617
Activity:
RAD51 inhibitor
Chemical Name:
3-Chloro-1-(3,4-dichlorophenyl)-4-(4-morpholinyl)-1H-pyrrole-2,5-dione
Molecular Weight:
361.61
Molecular Formula:
C14H11Cl3N2O3 Solubility:
Soluble in DMSO (up to 45 mg/ml) or in Ethanol (up to 10 mg/ml with warming)
Physical Properties:
Yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.
Shipping Code:
RT
更多产品咨询联系 上海惠诚生物 联系人:任荣 电话:18017273415