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| | 4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide Basic information |
| | 4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide Chemical Properties |
| density | 1.680±0.06 g/cm3(Predicted) | | storage temp. | room temp | | solubility | DMSO: ≥10mg/mL | | form | powder | | pka | 10.16±0.30(Predicted) | | color | off-white to light tan | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. | | InChIKey | VBOWCZDVEOFGRY-UHFFFAOYSA-N | | CAS DataBase Reference | 312756-74-4 |
| Hazard Codes | Xi | | Risk Statements | 36 | | Safety Statements | 26 | | WGK Germany | 3 |
| | 4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide Usage And Synthesis |
| Description | RS-1 is an activator of DNA repair protein RAD51 (Kd = 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. | | Uses | 4-Bromo-N-(4-bromophenyl)-3-[[(phenylmethyl)amino]sulfonyl]benzamide is a stimulant of the human homologous recombination protein RAD51. | | Uses | RS-1 has been shown to enhance CRISPR genome editing efficiency. To see other small molecule CRISPR enhancers, visit sigma.com/CRISPR-enhancers. | | General Description | 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. | | Biological Activity | 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. | | storage | Room temperature | | References | 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 Preparation Products And Raw materials |
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