Mdivi-1

製品コードS7162 バッチS716205

化学情報

	Synonyms	Mitochondrial division inhibitor 1	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₅H₁₀Cl₂N₂O₂S
	分子量	353.22	CAS No.	338967-87-6
Solubility (25°C)*	体外	DMSO	71 mg/mL (201.0 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Mdivi-1 (Mitochondrial division inhibitor 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. Mdivi-1 attenuates mitophagy and enhances apoptosis.
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]
特徴	The first selective inhibitor of mitochondrial division dynamins.

プロトコル(参考用のみ)

キナーゼアッセイ	GTP hydrolysis
キナーゼアッセイ	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.
動物実験	動物モデル	Male Sprague Dawley rats
	投薬量	3 mg/kg
	投与方法	IP injection

参考

カスタマーフィードバック

: , , Neurochem Res, 2017, 42(5):1449-1458

: Data from [Data independently produced by , , Blood Cancer J, 2017, doi:10.1038/bcj.2017.61]

: Data from [Data independently produced by , , Cell Physiol Biochem, 2017, 42(5):1802-1811]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Signaling via a CD27-TRAF2-SHP-1 axis during naive T cell activation promotes memory-associated gene regulatory networks [ Immunity, 2024, 57(2):287-302.e12]	PubMed: 38354704
Gonococcal OMV-delivered PorB induces epithelial cell mitophagy [ Nat Commun, 2024, 15(1):1669]	PubMed: 38396029
The DNA-dependent protein kinase catalytic subunit exacerbates endotoxemia-induced myocardial microvascular injury by disrupting the MOTS-c/JNK pathway and inducing profilin-mediated lamellipodia degradation [ Theranostics, 2024, 14(4):1561-1582]	PubMed: 38389837
Targeting PARP14 with lomitapide suppresses drug resistance through the activation of DRP1-induced mitophagy in multiple myeloma [ Cancer Lett, 2024, 588:216802]	PubMed: 38467180
PDGF-BB accelerates TSCC via fibroblast lactates limiting miR-26a-5p and boosting mitophagy [ Cancer Cell Int, 2024, 24(1):5]	PubMed: 38169376
Mitochondrial Responses to Sublethal Doxorubicin in H9c2 Cardiomyocytes: The Role of Phosphorylated CaMKII [ Yonago Acta Med, 2024, 4;67(1):41-51.]	PubMed: 38371275
Pathologically high intraocular pressure induces mitochondrial dysfunction through Drp1 and leads to retinal ganglion cell PANoptosis in glaucoma [ Redox Biol, 2023, 62:102687]	PubMed: 36989574
Attenuation of PM2.5-induced alveolar epithelial cells and lung injury through regulation of mitochondrial fission and fusion [ Part Fibre Toxicol, 2023, 20(1):28]	PubMed: 37464447
Attenuation of PM2.5-induced alveolar epithelial cells and lung injury through regulation of mitochondrial fission and fusion [ Part Fibre Toxicol, 2023, 20(1):28]	PubMed: 37464447
Endoplasmic reticulum-mitochondrial calcium transport contributes to soft extracellular matrix-triggered mitochondrial dynamics and mitophagy in breast carcinoma cells [ Acta Biomater, 2023, S1742-7061(23)00452-X]	PubMed: 37541606

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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