Mdivi-1 338967-87-6

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Molecular Weight:

353.22 Mdivi-1 is a selective Cell-Permeable Inhibitor of mitochondrial division DRP1 (Dynamin-Related Gtpase) and mitochondrial division Dynamin I (Dnm1) with IC50 of 1-10 μM.


Biological Activity


Mdivi-1
is a cell-permeable quinazolinone compound that inhibits yeast (Dnm1)
and mammalian (Drp1) division DRPs (dynamin-related GTPases) and
effectively induces mitochondrial fusion into net-like structures in a
reversible manner. Cell-free studies indicate that mdivi-1 blocks Dnm1
ATPase activity


Drp1 and GFAP protein expression is significantly increased in the early
neurodegenerative events of ischemic mouse retina. Mdivi-1 treatment
blocks apoptotic cell death in ischemic retina, and significantly
increases RGC survival at 2 weeks after ischemia. In the normal mouse
retina, Drp1 is expressed in the ganglion cell layer (GCL) as well as
the inner plexiform layer, the inner nuclear layer (INL), and the outer
plexiform layer (OPL). In the GCL, Drp1 immunoreactivity is strong in
RGCs. While Drp1 protein expression is increased in the GCL of
vehicle-treated ischemic retina at 12 hours. Mdivi-1 treatment does not
change this increase of Drp1 protein expression but significantly
decreased GFAP protein expression.


Protocol(Only for Reference)


Kinase Assay:


[1]

GTP hydrolysis

For determination of the kinetic parameters, GTPase assays are carried out in 25 mM HEPES, 25 mM PIPES, pH 7, 150 mM NaCl, 30 mM imidazole, pH 7.4, 7.5 mM KCl, 5 mM MgCl2, 1 mM phospho(enol)pyruvate (PEP), 20 U/mL pyruvate kinase/lactate dehydrogenase, 4% dimethyl sulfoxide (DMSO), and 600 μM NADH. Chemical inhibitor and GTP concentrations are varied, as specified. GTPase assay reactions are started by addition of approximately 10 μg of purified protein, in freezing buffer, to the GTPase assay reaction buffer containing the small molecule.

Animal Study:


[2]

Animal Models	C57BL/6 mice
Formulation	dimethyl sulfoxide [DMSO]
Dosages	50 mg/kg
Administration	IP injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	353.22
Formula	C15H10Cl2N2O2S
CAS No.	338967-87-6

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	N/A

Solubility (25°C) *	In vitro	DMSO	70 mg/mL (198.17 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	4(1H)-Quinazolinone, 3-(2,4-dichloro-5-methoxyphenyl)-2,3-dihydro-2-thioxo-

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Product Categories : Cytoskeletal Signaling > Dynamin Inhibitor