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Formula | C15H10Cl2N2O2S |
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Molecular Weight | 353.22 | CAS No. | 338967-87-6 | ||||||||
Solubility (25°C)* | In vitro | DMSO | 71 mg/mL (201.0 mM) | ||||||||
Water | Insoluble | ||||||||||
Ethanol | Insoluble | ||||||||||
In vivo (Add solvents to the product individually and in order) |
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* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | 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. | ||
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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] |
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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] |
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Features | The first selective inhibitor of mitochondrial division dynamins. |
Animal Study: |
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, , 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]
Data from [Data independently produced by , , Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2307-2318]
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 |
MANF facilitates breast cancer cell survival under glucose-starvation conditions via PRKN-mediated mitophagy regulation [ Autophagy, 2024, 1-22.] | PubMed: 39147386 |
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 |
Rictor/mTORC2 signalling contributes to renal vascular endothelial-to-mesenchymal transition and renal allograft interstitial fibrosis by regulating BNIP3-mediated mitophagy [ Clin Transl Med, 2024, 14(5):e1686] | PubMed: 38769658 |
Targeting PARP14 with lomitapide suppresses drug resistance through the activation of DRP1-induced mitophagy in multiple myeloma [ Cancer Lett, 2024, 588:216802] | PubMed: 38467180 |
lncRNA Oip5-as1 inhibits excessive mitochondrial fission in myocardial ischemia/reperfusion injury by modulating DRP1 phosphorylation [ Cell Mol Biol Lett, 2024, 29(1):72] | PubMed: 38745296 |
PDGF-BB accelerates TSCC via fibroblast lactates limiting miR-26a-5p and boosting mitophagy [ Cancer Cell Int, 2024, 24(1):5] | PubMed: 38169376 |
Inhibition of OGG1 ameliorates pulmonary fibrosis via preventing M2 macrophage polarization and activating PINK1-mediated mitophagy [ Mol Med, 2024, 30(1):72] | PubMed: 38822247 |
Deciphering the neuroprotective mechanisms of RACK1 in cerebral ischemia-reperfusion injury: Pioneering insights into mitochondrial autophagy and the PINK1/Parkin axis [ CNS Neurosci Ther, 2024, 30(8):e14836] | PubMed: 39097918 |
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