MG-132 - Proteasome 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMG-132Cat. No.: HY-13259CAS No.: 133407-82-6分式: CHNO分量: 475.62作靶點: Proteasome; Autophagy作通路: Metabolic Enzyme/Protease; Autophagy儲存式: 4C, protect from light* 該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使。溶解性數(shù)據(jù)體外實驗 DMSO : 83.33 mg/mL (175.20 mM; Need u

2、ltrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.37 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.37 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 MG-132種多肽醛，也 有效的，可逆的，可透過細胞的蛋酶體抑制劑，IC50 值為 100 nM

3、，有效地阻斷了 26S 蛋酶體復(fù)合物的蛋解活性 1 2。IC50 & Target IC50: 100 nM (Proteasome) 1體外研究 MG-132 (10-40 M; 24 hours) significantly reduces the viability of C6 glioma cells in both time- andconcentration-dependent manners and shows the IC50 of 18.5 M at 24 hours 3.MG-132 (18.5 M; 24 hours) induces down-regulation of

4、 anti-apoptotic proteins Bcl-2 and XIAP and up-regulates expression of pro-apoptotic protein Bax and caspase-3 3.Cell Viability Assay 3Cell Line: C6 glioma cellsConcentration: 10, 20, 30, 40 MIncubation Time: 24 hoursResult: Significantly reduced the viability of C6 glioma cells beginning at 6 h in

5、both time- andconcentration-dependent manners and showed the IC50 of 18.5 M at 24 hours.Western Blot Analysis 3Cell Line: C6 glioma cellsConcentration: 18.5 MIncubation Time: 24 hoursResult: Induced down-regulation of anti-apoptotic proteins Bcl-2 and XIAP, up-regulatedexpression of pro-apoptotic pr

6、otein Bax and caspase-3.體內(nèi)研究 MG-132 (1 mg/kg; i.v.; twice a week for 4 weeks) shows potent tumor inhibitory effect against mice bearingHeLa tumors 4.Animal Model: Five-week-old female C.B-17/lcr-scid/scidJcl mice (bearing HeLa cells) 4Dosage: 1 mg/kgAdministration: Intravenous injection; twice a wee

7、k for 4 weeksResult: The growth inhibition rates in HeLa tumors was 49% compared to the control.戶使本產(chǎn)品發(fā)表的科研獻 Adv Sci (Weinh). 2019 Mar 25;6(10):1801862. EMBO J. 2019 Feb 20. pii: e100376.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Nucleic Acids Res. 2018 Apr 20;46(7):3284-3297. Cancer Res. 2019

8、 May 1;79(9):2257-2270. Cancer Res. 2019 Feb 1;79(3):534-545.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Harhouri K, et al. MG132-induced progerin clearance is mediated by autophagy activation and splicing regulation. EMBO Mol Med. 2017Sep;9(9):1294-1313.2. Han YH, et al. T

9、he effect of MG132, a proteasome inhibitor on HeLa cells in relation to cell growth, reactive oxygen species and GSH.Oncol Rep. 2009 Jul;22(1):215-21.3. Fan WH, et al. Proteasome inhibitor MG-132 induces C6 glioma cell apoptosis via oxidative stress. Acta Pharmacol Sin. 2011May;32(5):619-25.4. Matsu

10、moto Y, et al. Enhanced efficacy against cervical carcinomas through polymeric micelles physically incorporating theproteasomeinhibitor MG132. Cancer Sci. 2016 Jun;107(6):773-81.5. Chen B, et al. MG132, a proteasome inhibitor, attenuates pressure-overload-induced cardiac hypertrophy in rats by modulation ofmitogen-activated protein kinase signals. Acta Biochim Biophys Sin (Shanghai). 2010 Apr;42(4):253-8.McePdfHeightCaution: Product has not been full