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

4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide
  • CAS No.:312756-74-4

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  1. This product is a chemical product/pharmaceutical intermediate. It is not a drug, an active pharmaceutical ingredient (API), or a pharmaceutical-grade material. It has not been granted a drug approval number or a Chemical Drug Substance Approval Notice, has not passed drug-related review and approval, and is not manufactured, tested, or released in accordance with pharmaceutical GMP.
  2. This product is intended solely for non-clinical research, process development, quality studies, further chemical processing, or chemical synthesis. It must not be used in drug-product manufacturing, clinical trials, clinical diagnosis, or administration to humans or animals, or be sold, used as an input, submitted for regulatory filing, or released as an API or pharmaceutical material.
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4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide Basic information
Product Name:4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide
Synonyms:4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide;RAD51-Stimulatory Compound-1, RS-1;RAD51-stimulatory compound 1;RS-1;CS-2312;RS1;RS 1;RS-1 - RAD51-Stimulatory Compound-1;3-benzylsulfamoyl-4-bromo-N-(4-bromophenyl)benzamide
CAS:312756-74-4
MF:C20H16Br2N2O3S
MW:524.23
EINECS:
Product Categories:API;Amines, Aromatics, Pharmaceuticals, Intermediates & Fine Chemicals
Mol File:312756-74-4.mol
4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide Chemical Properties
storage temp. room temp
solubility DMSO: ≥10mg/mL
form powder
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.
InChIKeyVBOWCZDVEOFGRY-UHFFFAOYSA-N
CAS DataBase Reference312756-74-4
Safety Information
Hazard Codes Xi
Risk Statements 36
Safety Statements 26
WGK Germany 3
MSDS Information
4-BroMo-N-(4-broMophenyl)-3-[[(phenylMethyl)aMino]sulfonyl]benzaMide Usage And Synthesis
DescriptionRS-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.
Uses4-Bromo-N-(4-bromophenyl)-3-[[(phenylmethyl)amino]sulfonyl]benzamide is a stimulant of the human homologous recombination protein RAD51.
UsesRS-1 has been shown to enhance CRISPR genome editing efficiency. To see other small molecule CRISPR enhancers, visit sigma.com/CRISPR-enhancers.
General DescriptionA 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 ActivityRS-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 ActionsRS-1 is a sulfonamido-benzamide compound.
in vitroRS-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.
References1) 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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