Description |
Mdivi-1 is a selective dynamin-related protein 1 (Drp1) inhibitor.
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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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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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Density | 1.6±0.1 g/cm3 |
Boiling Point | 522.5±60.0 °C at 760 mmHg |
Flash Point | 269.8±32.9 °C |
Exact Mass | 351.984009 |
PSA | 82.92000 |
LogP | 3.85 |
Vapour Pressure | 0.0±1.4 mmHg at 25°C |
Storage condition | Store at -20°C |