化合物RI1 T2276

Product Introduction
Bioactivity


英文名: RI-1

描述: RI-1 (RAD51 inhibitor 1) 是一种选择性 RAD51的抑制剂，IC50值为 5-30 μM，可以破坏人类细胞中的同源重组。它在半胱氨酸 319 处与 RAD51 蛋白表面共价结合，并通过直接结合到 RAD51 细丝中蛋白质亚基之间的界面的蛋白质表面来灭活 RAD51。

细胞实验: Cytotoxicity is determined by loss of colony-forming ability. Experiments are performed in triplicate. Crystal violet stained colonies are imaged with a CCD camera and counted using NIH Image software. Error bars denote standard error.(Only for Reference)

激酶实验: DNA binding assays: All reactions are performed in black non-binding polystyrene 384-well plates with reaction volumes of 30–100 μL. Purified DNA strand exchange proteins and chemical compounds are pre-incubated at room temperature for 5 minutes; they are then further incubated at 37°C for 30 min with 100 nM of ssDNA substrate, consisting of a 45-mer poly-dT tagged with Alexa 488 at the 5' terminus (synthesized and purified by Integrated DNA Technologies). Reactions are performed in 20 mM HEPES pH 7.5, 10 mM MgCl2, 0.25 μM BSA, 2% glycerol, 30 mM NaCl, 4% DMSO and 2 mM ATP. Some conditions included DTT or TCEP (tris(2-carboxyethyl)phosphine) as indicated. DNA binding is measured as a function of fluorescence polarization (FP) with a Safire2 plate reader, using the following settings: excitation 470±5 nM, emission 530±5 nM, 10 reads/well, Z height and G factor auto-calibrated from control wells. Displayed error bars represent standard deviation. For experiments involving a titration of protein concentrations, data are fit to an equation that accounts for the cooperative nature by which recombinase proteins bind DNA. For experiments involving a titration of RI-1, protein concentrations are selected to give an ～80% saturation of the FP signal in the absence of RI-1.

体内活性: 在HeLa细胞,MCF-7和U2OS三种癌细胞株中,RI-1具有单剂毒性（LD50：20-40 μM）。 通过直接和特异破坏HsRAD51和抑制RAD51,RI-1可抑制RAD51在ssDNA上形成丝的能力,从而使细胞对DNA损伤的敏感性增加。RI-1使G2期细胞的γ-H2AX灶减少,并使辐射6小时后未修复DSB的水平增加。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 36.2 mg/mL (100 mM)


关键字: recombination | homologous | RI 1 | Inhibitor | RAD51 | inhibit | RI-1

相关产品: Danofloxacin | Dmt-2'fluoro-da(bz) amidite | Beaucage reagent | L67 | Trimethoprim | Werner syndrome RecQ helicase-IN-1 | RNase L-IN-1 | T7 RNA polymerase | SMN-C2 | Folinic acid calcium

相关库: Anti-Aging Compound Library | Cell Cycle Compound Library | Anti-Cancer Compound Library | Toxic Compound Library | Bioactive Compounds Library Max | Inhibitor Library | DNA Damage & Repair Compound Library | NO PAINS Compound Library | Bioactive Compound Library

化合物RI1 T2276信息由TargetMol中国为您提供，如您想了解更多关于化合物RI1 T2276报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途