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Mdivi-1

CAS No. : 338967-87-6

MCE 站：Mdivi-1

产品活性：Mdivi-1 是选择性的发动蛋白相关蛋白 1 (Drp1) 抑制剂。Mdivi-1 是一种有效的线粒体分裂/线粒体自噬 (mitophagy) 抑制剂。

研究领域：Cytoskeleton  |  Autophagy  |  Apoptosis

作用靶点：Dynamin  |  Mitophagy  |  Autophagy  |  Apoptosis

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 K_0.5 for GTP, lowers the apparent V_max for GTP hydrolysis, and causes an increase in the Hill coefficient observed for GTP in the Dnm1 GTP hydrolysis reaction. 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.?Mdivi-1 results in apoptotic cell death in ischemic retina.

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. Mdivi-1 (50 mg/kg, i.p.) significantly decreases GFAP protein expression in the normal mouse retina.

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