PRT4165-NSC600157-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPRT4165Cat. No.: HY-19817CAS No.: 31083-55-3Synonyms: NSC600157分式: CHNO分量: 235.24作靶點(diǎn): E1/E2/E3 Enzyme作通路: Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 25 mg/mL (

2、106.27 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (10.63 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (10.63 mM); Suspended solution; Need ultrasonic1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑： 10% D

3、MSO 90% corn oilSolubility: 2.5 mg/mL (10.63 mM); Precipitated solutionBIOLOGICAL ACTIVITY物活性 PRT4165種有效的 PRC1 介導(dǎo)的 H2A 泛素化的抑制劑。IC50 & Target PRC1 1體外研究 PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation. In vitro E3 ubiquitin ligase activityassays reveal that PRT4165 inhibits both RNF

4、2 and RING 1A, but not RNF8 nor RNF168. In the presence ofPRT4165, H2A ubiquitylation could be completely inhibited regardless of whether RING1 or RNF2contributes the E3 ubiquitin ligase activity. Treatment of cells for 60 min with 50 M PRT4165 results in adramatic reduction in total ubiquitylated h

5、istone H2A. It is also found that longer exposure of the cells with thePRT4165 (30 and 60 min) leads to increased levels of -H2AX in unirradiated cells. PRT4165 inhibits double-strand break (DSB) repair at the 8-h time point compare with mock treated cells. Cells treated with increasingconcentration

6、s of PRT4165 show increasing numbers of cells in G2/M 1.PROTOCOLCell Assay 1 Cells are treated with different concentrations of the PRT4165 60 min prior to irradiation (2 Gy). The cells areharvested 2 h after IR. The cells are washed with PBS twice and then fixed with 1% paraformaldehyde at37C for 1

7、0 min. After cooling on ice for 1 min, the cells are permeabilized with 90% methanol and stored at -20C overnight. Fixed cells are washed with PBS twice and blocked with FACS incubation buffer (0.5% BSAin PBS) for 10 min. The cells are then stained with anti-phosphohistone H3 (serine 10) antibody at

8、 1:500dilution in FACS incubation buffer for 1 h at room temperature 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cancer Res. 2018 Jan 1;78(1):51-63.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Ismail IH, et al. A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks. JBiol Chem. 2013 Sep 13;288(37):26944-54.McePdfHeightCaution: Product has not been fully validated for medical appl