Antibodies
Mdivi-1
- 貨號 Cat. No.
- S7162
- 規格 Size
- 20mgã€50mg
- 品牌 Brand
- Selleckchem
Description
Mdivi-1
Catalog No.S7162
Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial divisionDynamin I (Dnm1) with IC50 of 1-10 μM.
| Size | Price | Stock | Quantity | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| |||||||||||
Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | 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. | |||||
|---|---|---|---|---|---|---|
| Targets | Dynamin I | |||||
| IC50 | 1-10 μM[1] | |||||
| In vitro | 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 (IC50<10 μM) and self-assembly by an allosteric modulation-based mechanism. Mdivi-1 is shown to effectively suppress STS- as well as C8-Bid-induced MOMP (Mitochondrial Outer Membrane Permeabilization) in HeLa cultures and in cell-free murine liver mitochondria preparations, respectively, as assessed by cytochrome C release. In cells, mdivi-1 retards apoptosis by inhibiting mitochondrial outer membrane permeabilization. In principle, mivi-1 represents a class of therapeutics for stroke, myocardial infarction, and neurodegenerative diseases. [1] | |||||
| In vivo | 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. [2] | |||||
| Features | The first selective inhibitor of mitochondrial division dynamins. | |||||
Protocol(Only for Reference)
Kinase Assay:
| 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:
| Animal Models | C57BL/6 mice |
|---|---|
| Dosages | 50 mg/kg |
| Administration | IP injection |
References
Chemical Information
| Molecular Weight (MW) | 353.22 |
|---|---|
| Formula | C15H10Cl2N2O2S |
| CAS No. | 338967-87-6 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 71 mg/mL (201 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <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- |
|---|
