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Drp1 inhibitor SC9

Chemical Structure : Drp1 inhibitor SC9

CAS No.: 851471-44-8

Drp1 inhibitor SC9 (Drp1 SWAG ligand SC9)

Catalog No.: PC-20940Not For Human Use, Lab Use Only.

Drp1 inhibitor SC9 (Drp1 SWAG ligand SC9) is a small molecule binder of dynamin-related protein 1 (Drp1) allosteric site switch I-adjacent groove (SWAG), inhibits GTPase activity of Drp1 (IC50=270 nM) and inhibits Drp1-Fis1 interaction in cells.

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    Biological Activity

    Drp1 inhibitor SC9 (Drp1 SWAG ligand SC9) is a small molecule binder of dynamin-related protein 1 (Drp1) allosteric site switch I-adjacent groove (SWAG), inhibits GTPase activity of Drp1 (IC50=270 nM) and inhibits Drp1-Fis1 interaction in cells.
    SC9 act as uncompetitive inhibitors of WT Drp1, SC9 (1 uM) reduced both Km and Vmax of Drp1.
    SC9 reduces LPS-induced mitochondrial dysfunction in H9c2 cells.
    SC9 blocks stress-induced Drp1 oligomerization, inhibits LPS-induced mitochondrial membrane depolarization in H9c2 cells with IC50 of 750 nM.
    SC9 blocks mitochondrial translocation of Drp1 to the mitochondria by selectively inhibiting Drp1-Fis1 interaction.
    SC9 (10 mg/kg, i.p.) effectively inhibits LPS-induced mortality in mouse model of endotoxemia.

    Physicochemical Properties

    M.Wt 466.52
    Formula C21H22N8O3S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    N-(6-amino-1-benzyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-2-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)thio)-N-methylacetamide

    References

    1. Rios L, et al. Nat Commun. 2023 Jul 19;14(1):4356.

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