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Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1). DRP1, a member of the dynamin family of large GTPases, mediates mitochondrial fission.
In vitro: The most efficacious inhibitor, mdivi-1 attenuates mitochondrial division in yeast and mammalian cells by selectively inhibiting the mitochondrial Drp1-mediated division dynamin. Mdivi-1 potently blocks Bid-activated Bax/Bak-dependent cytochrome c release from mitochondria [1].
In vivo: Mdivi-1 treatment blocked apoptotic cell death in ischemic retina, and significantly increased RGC survival at 2 weeks after ischemia. Moreover, Mdivi-1 treatment did not change this increase of Drp1 protein expression but significantly decreased GFAP protein expression [2].
Clinical trial: Currently no clinical data are available.
References:[1] Cassidy-Stone A, Chipuk JE, Ingerman E, Song C, Yoo C, Kuwana T, Kurth MJ, Shaw JT, Hinshaw JE, Green DR, Nunnari J. Chemical inhibition of the mitochondrial division dynamin reveals its role in Bax/Bak-dependent mitochondrial outer membrane permeabilization. Dev Cell. 2008;14(2):193-204. [2] Park SW, Kim KY, Lindsey JD, Dai Y, Heo H, Nguyen DH, Ellisman MH, Weinreb RN, Ju WK. A selective inhibitor of drp1, mdivi-1, increases retinal ganglion cell survival in acute ischemic mouse retina. Invest Ophthalmol Vis Sci. 2011;52(5):2837-43.
Cell lines
Yeast cells harboring the temperature-sensitive fzo1-1 allele
Preparation method
The solubility of this compound in DMSO is >17.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition
50 μM
Applications
Mdivi-1 (50 μM) inhibited mitochondrial division in mammalian cells (COS cells) by attenuating Drp1 self-assembly. Mdivi-1 (50 μM) attenuated mammalian mitochondrial division and Drp1 self-assembly during apoptosis. Mdivi-1 significantly inhibited STS-induced annexin V staining of non-necrotic cells as assessed by FACS analysis, indicating that mdivi-1 inhibited apoptosis.
Animal models
C57BL/6 mice
Dosage form
Intraperitoneal injection, 50 mg/kg, 60 minutes
Application
Mdivi-1 treatment significantly increased RGC survival by approximately 54% in the central, 58% in the middle, and 48% in the peripheral areas. Mdivi-1 treatment significantly decreased GFAP protein expression in ischemic retina at 12 hours. Mdivi-1 treatment did not change mean arterial blood pressure, body weight, animal appearance or behavior.
Other notes
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References:
[1]. Cassidy-Stone A, Chipuk J E, Ingerman E, et al. Chemical inhibition of the mitochondrial division dynamin reveals its role in Bax/Bak-dependent mitochondrial outer membrane permeabilization[J]. Developmental cell, 2008, 14(2): 193-204.
[2]. Park S W, Kim K Y, Lindsey J D, et al. A selective inhibitor of drp1, mdivi-1, increases retinal ganglion cell survival in acute ischemic mouse retina[J]. Investigative ophthalmology & visual science, 2011, 52(5): 2837-2843.
