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Description: PF429242 dihydrochloride is a novel, potent, reversible and competitive S1P sterol regulatory element-binding protein (SREBP) site 1 protease inhibitor with an IC50 of 170 nM. PF 429242 showed no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 uM and only modest inhibition of urokinase (IC50 = 50 uM) and factor Xa (IC50 = 100 uM). PF-429242 is selective for site 1 protease against a panel of serine proteases. PF-429242 inhibits rate of cholesterol synthesis in CHO cells with IC50 of 0.53 uM.
References: J Pharmacol Exp Ther. 2008 Sep; 326(3):801-8.; Viruses. 2016 Feb 10; 8(2). pii: E46.; J Virol. 2011 Jan; 85(2):795-803.
Related CAS#:947303-87-9 (free base)
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