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Fig. 2 | BMC Pharmacology and Toxicology

Fig. 2

From: Ethacrynic acid is an inhibitor of human factor XIIIa

Fig. 2

Effect of EA on FXIIIa-mediated fibrin(ogen) polymerization. A The effect of EA on FXIIIa-mediated fibrin polymerization was investigated by SDS-PAGE. Different concentrations of EA (5 – 5000 µM) were used. The figure shows that EA concentration dependently inhibited the formation of γ–γ (dimers; about 117 kDa) as well as α–α (larger polymers; > 250 kDa). B The dose–response curves for the formation of dimers and polymers from which the inhibition parameters were deduced using Eq. 1. EA inhibited the formation of the γ–γ dimers with an IC50 value of ~ 1176.8 µM and an efficacy of ~ 94.7%, yet it was more potent inhibiting the formation of the larger polymers of α – α with and an IC50 value of ~ 120.1 µM and an efficacy of ~ 81.6%. This shows that EA not only inhibiting FXIIIa activity using non-physiological substrates (N,N-dimethylcasein and dansylcadaverine) but also using its physiological substrates (α-, β-, and γ- fibrin(ogen)) monomers. Original gels are provided in the supplementary information. The edges were removed to provide better clarity. Experiment was repeated three times

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