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

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H319：Verursacht schwere Augenreizung.

• Sicherheit

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  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.

• Verwenden

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

• Verwenden

  RS-1 has been shown to enhance CRISPR genome editing efficiency. To see other small molecule CRISPR enhancers, visit sigma.com/CRISPR-enhancers.

• Allgemeine Beschreibung

  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.

• Biologische Aktivität

  RS-1 is a RAD51-stimulatory compound, which increases the DNA binding activity of RAD51. It is an HDR(homology-directed repair) enhancer that enhances Cas9- and TALEN-mediated knock-in efficiency in rabbit embryos both in vitro and in vivo.

• Biochem/physiol Actions

  RS-1 is a sulfonamido-benzamide compound.

• in vitro

  RS-1 stimulates the binding of hRAD51 to ssDNA. Low-micromolar concentrations of this small molecule enhance DNA binding and result in longer protein–DNA complex lengths. In addition, RS-1 stabilizes the active form of hRAD51 filaments and this is reflected in an enhanced strand assimilation activity[1]. RS-1 enhances Cas9- and TALEN-mediated knock-in efficiency in rabbit embryos both in vitro and in vivo.

• Lager

  Room temperature

• Einzelnachweise

  1) Jayathilaka et al. (2008), A chemical compound that stimulates the human homologous recombination protein RAD51; Proc. Natl. Acad. Sci. USA 105 15848 2) Mason et al. (2014), The RAD51-stimulatory compound RS-1 can exploit the RAD51 overexpression that exists in cancer cells and tumors; Cancer Res. 74 3546 3) Pinder et al. (2015), Nuclear domain ‘knock-in’ screen for the evaluation and identification of small molecule enhancers of CRISPR-based genome editing; Nucleic Acids Res. 43 9379 4) Song et al. (2016), RS-1 enhances CRISPR/Cas9- and TALEN-mediated knock-in efficiency; Nat. Commun. 7 10548

4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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