Drp1 inhibitor SC9 | Drp1 inhibitor | Probechem Biochemicals

Chemical Structure : Drp1 inhibitor SC9

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Drp1 inhibitor SC9 (Drp1 SWAG ligand SC9)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	466.52
分子式	C21H22N8O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

Drp1 inhibitor SC9 (Drp1 SWAG ligand SC9)

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物理化学性质&存储条件

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Drp1 inhibitor SC9 (Drp1 SWAG ligand SC9)

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物理化学性质&存储条件

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