4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide

Описание

RS-1 is an activator of DNA repair protein RAD51 (K_d = 48-107 for human RAD51 with different cofactors present). It stimulates homologous strand assimilation activity at least 5- to 11-old, enhancing homologous recombination activity of hRAD51. RS-1 is a potent enhancer of CRISPR-mediated genome editing, increasing homology directed repair 3- to 6-fold. It is used to increase CRISPR-mediated knock-in efficiencies in vitro and in vivo.

Использование

4-Bromo-N-(4-bromophenyl)-3-[[(phenylmethyl)amino]sulfonyl]benzamide is a stimulant of the human homologous recombination protein RAD51.

Общее описание

A cell-permeable sulfonamido-benzamide-based allosteric regulator that stimulates DNA binding and recombinase activities of hRAD51 by locking hRAD51 in an active conformation without affecting its active site ATP hydrolysis. Although RS-1 enhances hRAD51 filament formation on ssDNA with or without the cofactor NTP, active filaments and recombinase activity are only induced in the presence of ATP or AMP-PNP, but not with ADP or no cofactors. Shown to promote resistance of primary human neonatal dermal fibroblasts to Cisplatin- (Cat. No. 232120) induced death in a dose-dependent manner. RS-1 is inactive toward related DNA strand exchange proteins scRAD5 and scDMC1 of yeast origin or E. coli RedA.This HDR (homology-directed repair) enhancer, is shown to significantly increase both Cas9 & TALEN-mediated knock-in efficiencies.