Mdivi-1-Mitochondrial-division-inhibitor-1-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMdivi-1Cat. No.: HY-15886CAS No.: 338967-87-6Synonyms: Mitochondrial division inhibitor 1分式: CHClNOS分量: 353.22作靶點: Dynamin; Mitophagy作通路: Cytoskeleton; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mo

2、nth溶解性數(shù)據(jù)體外實驗 DMSO : 32 mg/mL (90.60 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.08 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (7.08 mM); Suspended solution; Need ultrasonic3. 請依序添加每

3、種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.08 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Mdivi-1選擇性的發(fā)動蛋相關(guān)蛋 1 (Drp1) 抑制劑。Mdivi-1 種有效的線粒體分裂/線粒體噬 (mitophagy) 抑制劑。體外研究 Mdivi-1 inhibits Dnm1 GTPase activity in a dose-dependent manner, with an estimated EC50 of 1-10 M.Mdivi-1 increases the apparent

4、 K0.5 for GTP, lowers the apparent Vmax for GTP hydrolysis, and causes anincrease in the Hill coefficient observed for GTP in the Dnm1 GTP hydrolysis reaction 1. Cells treated withmdivi-1 display decreased cytochrome c release and a reduced rate of phosphatidylserine exposure on theirsurface followi

5、ng apoptosis induction, consistent with an inhibition of apoptosis and with previous studiesusing other strategies to compromise DRP1 activity 2. Mdivi-1 results in apoptotic cell death in ischemicretina 3.體內(nèi)研究 The mitochondrial division DRP, Dnm1, is the target of mdivi-1 in vivo. Mdivi-1 quantitat

6、ively blocksGMPPCP- dependent Dnm1 self-assembly in a concentration range similar to its effects on mitochondrialdivision in vivo 1. Mdivi-1 (50 mg/kg, i.p.) significantly decreases GFAP protein expression in the normalmouse retina 3.PROTOCOLKinase Assay 1 All GTPase assay reactions are started in a

7、 200 L volume, of which 150 L is placed into the well of a 96-well plate. Depletion of NADH, as monitored by reading the A340 of the reaction, is measured every 20 s fora total of 40 min using a SpectraMAX 250 96-well plate reader. Spectrophotometric data are transferred toExcel and the measured ste

8、ady state depletion of NADH over time is converted to protein activity.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 YPGlycerol plates are topped with 10 mL YPGlycerol containing 1% low melt agar and 75 M mdivi-1, andcells are spotted 12

9、hours later using a 48 well pinning device. After pinning cells, plates are incubated at24C or 37C and imaged using an Eagle Eye II imaging system.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) J Pineal Res. 2018 Sep;65(2):e12491. J Pineal

10、Res. 2018 Jan;64(1). Theranostics. 2019 Feb 28;9(6):1698-1713. PLoS Pathog. 2016 Aug 24;12(8):e1005823. Cell Death Dis. 2019 Mar 8;10(3):232.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Cassidy-Stone A, et al. Chemical inhibit

11、ion of the mitochondrial division dynamin reveals its role in Bax/Bak-dependent mitochondrialouter membrane permeabilization. Dev Cell. 2008 Feb;14(2):193-204.2. Tanaka A, et al. A chemical inhibitor of DRP1 uncouples mitochondrial fission and apoptosis. Mol Cell. 2008 Feb 29;29(4):409-10.3. Park SW, et al. A selective inhibitor of drp1, mdivi-1, increases retinal ganglion cell survival in acute ischemic mouse retina. InvestOphthalmol Vis Sci. 2011 Apr 27;52(5):2837-43.McePdfHeightCaution: Product