RS-1
(Synonyms: 4-溴-N-(4-溴苯基)-3-[[(苯基甲基)氨基]磺酰基]苯甲酰胺) 目录号 : GC16265
A RAD51 activator
Cas No.:312756-74-4
Sample solution is provided at 25 µL, 10mM.
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RS-1 is a stimulatory compound of RAD51, a key player in the HR complex. RS-1 could increase the DNA binding activity of RAD51 and function in vivo to enhance the homologous recombination activity of hRAD51 by promoting the formation of active presynaptic filaments [1].
The hRAD51 protein could bind with single- and double-stranded DNA and exhibit DNA-dependent ATPase activity. Rad51 mediates homology recognition and initiates strand exchange [2]. Chromosome analysis revealed that Rad51‐deficient vertebrate cells accumulated chromosomal breaks in the G2/M phase of the cell cycle prior to cell death. Rad51 played an essential role in the repair of spontaneously occurring chromosome breaks in proliferating cells of higher eukaryotes [3].
RS-1 treatment promoted significant antitumor responses in a mouse mode. It can be used to kill human cancer cells, and that its toxicity is modulated by both RAD51 and RAD54 translocase expression levels [4]. RS-1 effectively improved the knock-in rates in the TALEN- and the Cas9-mediated genome-editing systems in rabbits. RS-1 showed little toxic effects on the overall animal health and reproduction. RS-1 enhanced Cas9- and TALEN-mediated knock-in efficiency in rabbit embryos both in vitro and in vivo. RS-1 treatment (15 μM) appeared to enhance the blastocyst development in embryos. Treating embryos with RS-1 at 7.5 μM resulted in 26.1% knock-in rate [5].
References:
[1]. Jayathilaka K, Sheridan S D, Bold T D, et al. A chemical compound that stimulates the human homologous recombination protein RAD51[J]. Proceedings of the National Academy of Sciences, 2008, 105(41): 15848-15853.
[2]. Baumann P, Benson F E, West S C. Human Rad51 protein promotes ATP-dependent homologous pairing and strand transfer reactions in vitro[J]. Cell, 1996, 87(4): 757-766.
[3]. Sonoda E, Sasaki M S, Buerstedde J M, et al. Rad51‐deficient vertebrate cells accumulate chromosomal breaks prior to cell death[J]. The EMBO journal, 1998, 17(2): 598-608.
[4]. Mason J M, Logan H L, Budke B, et al. The RAD51-stimulatory compound RS-1 can exploit the RAD51 overexpression that exists in cancer cells and tumors[J]. Cancer research, 2014, 74(13): 3546-3555.
[5]. Song J, Yang D, Xu J, et al. RS-1 enhances CRISPR/Cas9-and TALEN-mediated knock-in efficiency[J]. Nature communications, 2016, 7.
Kinase experiment: | Briefly, 15 μL reaction volumes include a DNA strand exchange protein (0.8 μM) that is preincubated for 5 min at 37°C with 1 μM (nucleotide concentration) 32P-labeled oligonucleotide 306.7 in a reaction buffer containing 20 mM Hepes (pH 7.5), 1 mM DTT, 2 mM nucleotide cofactor, and 1 mM MgCl2 and various concentrations of RS-1. For experimental buffer conditions that included calcium, 1 mM CaCl2 is present in addition to (in the case of hRAD51) or in the place of (in the case of RecA and scRAD51) the 1 mM MgCl2. Conditions with scRAD51 additionally contains 110 nM scRAD54. After this initial binding reaction, 10 μL of 19.75 μM (base pair concentration) supercoiled homologuecontaining target plasmid DNA (pRS306) is next added along with sufficient magnesium acetate to give a final concentration of 10 mM[1]. |
References: [1]. Jayathilaka K, et al. A chemical compound that stimulates the human homologous recombination protein RAD51. Proc Natl Acad Sci U S A. 2008 Oct 14;105(41):15848-53. | |
| Cas No. | 312756-74-4 | SDF | |
| 别名 | 4-溴-N-(4-溴苯基)-3-[[(苯基甲基)氨基]磺酰基]苯甲酰胺 | ||
| 化学名 | 4-bromo-N-(4-bromophenyl)-3-[[(phenylmethyl)amino]sulfonyl]-benzamide | ||
| Canonical SMILES | BrC1=CC=C(NC(C2=CC=C(Br)C(S(NCC3=CC=CC=C3)(=O)=O)=C2)=O)C=C1 | ||
| 分子式 | C20H16Br2N2O3S | 分子量 | 524.2 |
| 溶解度 | ≥ 20mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9077 mL | 9.5383 mL | 19.0767 mL |
| 5 mM | 0.3815 mL | 1.9077 mL | 3.8153 mL |
| 10 mM | 0.1908 mL | 0.9538 mL | 1.9077 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet