1. Product information
Names
| Name | 3-(2,4-dichloro-5-methoxyphenyl)-2-sulfanylidene-1H-quinazolin-4-one |
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| Synonym | More Synonyms |
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Mdivi-1 Biological Activity
| Description | Mdivi-1 is a selective dynamin-related protein 1 (Drp1) inhibitor. |
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| Related Catalog | Signaling Pathways >> Cytoskeleton >> Dynamin Research Areas >> Cancer |
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| In Vitro | Mdivi-1 inhibits Dnm1 GTPase activity in a dose-dependent manner, with an estimated EC50 of 1-10 μM. Mdivi-1 increases the apparent K0.5 for GTP, lowers the apparent Vmax for GTP hydrolysis, and causes an increase in the Hill coefficient observed for GTP in the Dnm1 GTP hydrolysis reaction[1]. Cells treated with mdivi-1 display decreased cytochrome c release and a reduced rate of phosphatidylserine exposure on their surface following apoptosis induction, consistent with an inhibition of apoptosis and with previous studies using other strategies to compromise DRP1 activity[2]. Mdivi-1 results in apoptotic cell death in ischemic retina[3]. |
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| In Vivo | The mitochondrial division DRP, Dnm1, is the target of mdivi-1 in vivo. Mdivi-1 quantitatively blocks GMPPCP- dependent Dnm1 self-assembly in a concentration range similar to its effects on mitochondrial division in vivo[1]. Mdivi-1 (50 mg/kg, i.p.) significantly decreases GFAP protein expression in the normal mouse retina[3]. |
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| Kinase Assay | All GTPase assay reactions are started in a 200 μL volume, of which 150 μL 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 for a total of 40 min using a SpectraMAX 250 96-well plate reader. Spectrophotometric data are transferred to Excel and the measured steady state depletion of NADH over time is converted to protein activity. |
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| Cell Assay | YPGlycerol plates are topped with 10 mL YPGlycerol containing 1% low melt agar and 75 μM mdivi-1, and cells are spotted 12 hours later using a 48 well pinning device. After pinning cells, plates are incubated at 24°C or 37°C and imaged using an Eagle Eye II imaging system. |
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| References | [1]. Cassidy-Stone A, et al. Chemical inhibition of the mitochondrial division dynamin reveals its role in Bax/Bak-dependent mitochondrial outer 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. Invest Ophthalmol Vis Sci. 2011 Apr 27;52(5):2837-43. [4]. Zhou K, et al. RIP1-RIP3-DRP1 pathway regulates NLRP3 inflammasome activation following subarachnoid hemorrhage. Exp Neurol. 2017 Sep;295:116-124. |
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Chemical & Physical Properties
| Density | 1.6±0.1 g/cm3 |
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| Boiling Point | 522.5±60.0 °C at 760 mmHg |
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| Melting Point | 289 °C |
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| Molecular Formula | C15H10Cl2N2O2S |
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| Molecular Weight | 353.223 |
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| Flash Point | 269.8±32.9 °C |
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| Exact Mass | 351.984009 |
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| PSA | 82.92000 |
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| LogP | 3.85 |
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| Vapour Pressure | 0.0±1.4 mmHg at 25°C |
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| Index of Refraction | 1.729 |
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| Storage condition | Store at -20°C |
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| Water Solubility | DMSO: >20mg/mL |
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Safety Information
| Hazard Codes | Xi |
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| RIDADR | NONH for all modes of transport |
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2. Packaging
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping
4. Contact information
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