GSK716 | Zα1-antitrypsin inhibitor | Probechem Biochemicals

Chemical Structure : GSK716

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GSK716 (GSK-716)

货号: PC-38247Not For Human Use, Lab Use Only.

GSK716 (GSK-716) is a potent inhibitor of Z α1-antitrypsin polymerisation, binds to Zα1-antitrypsin with a high-affinity (pKD=8.5).

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生物&药学活性

GSK716 (GSK-716) is a potent inhibitor of Z α1‐antitrypsin polymerisation, binds to Zα1‐antitrypsin with a high‐affinity (pKD=8.5).
GSK716 completely blocked the intracellular formation of Zα1‐antitrypsin polymers as measured by staining with the 2C1 anti‐Z α1‐antitrypsin polymer monoclonal antibody (pIC50=6.3).
GSK716 also increased the secretion of Z α1‐antitrypsin (pEC50=6.2). GSK716 exhibited a good level of selectivity over the off‐target panel and over other serpins.
GSK716 binds to a cryptic binding pocket, negate the local effects of the Z mutation and stabilise the bound state against progression along the polymerisation pathway.
GSK716 reduces intracellular polymerisation and increases the secretion of Z α1‐antitrypsin threefold in a transgenic mouse model of Z α1‐antitrypsin deficiency.

物理化学性质&存储条件

分子量	370.424
分子式	C21H23FN2O3
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-((1S,2R)-1-(3-fluoro-2-methylphenyl)-1-hydroxypentan-2-yl)-2-oxoindoline-4-carboxamide

参考文献

1. Lomas DA, et al. EMBO Mol Med. 2021 Mar 5;13(3):e13167.

GSK716 (GSK-716)

生物&药学活性

物理化学性质&存储条件

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GSK716 (GSK-716)

生物&药学活性

物理化学性质&存储条件

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