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Mdivi 1

In stock
Catalog No.
A4472
Selective DRP1/Dnm1 inhibitor, cell-permeable
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
10mg
$50.00
In stock
50mg
$200.00
In stock

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Email: [email protected]

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Background

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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt353.22
Cas No.338967-87-6
FormulaC15H10Cl2N2O2S
Solubility≥17.65mg/mL in DMSO, <2.434 mg/mL in EtOH, <2.12 mg/mL in H2O
Chemical Name3-(2,4-dichloro-5-methoxyphenyl)-2-sulfanylidene-1H-quinazolin-4-one
SDFDownload SDF
Canonical SMILESCOC1=C(C=C(C(=C1)N2C(=O)C3=CC=CC=C3NC2=S)Cl)Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

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 experiment [2]:

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.

Biological Activity

Description Mdivi 1 is a selective cell-permeable inhibitor of mitochondrial division dynamin-related GTPase (DRP1) and mitochondrial division dynamin I (Dnm1).
Targets DRP1 Dnm1        
IC50   1 - 10 µM        

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