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Beschreibung

A cell-permeable iodo-pyrimidine compound that covalently modifies MIF N-terminal proline and exhibits higher MIF inhibitory potency than ISO-1 (Cat. No. 475837) in cell-free dopachrome tautomerase activity assays (IC50 ~5 vs. 50 µ,M, respectively, using recombinant human MIF) as well as in cell-based migration assays (50% vs 0% inhibition with respective inhibitor at 10 µ,M) and anchorage-independent growth (57% vs 0% inhibition with respective inhibitor at 10 µ,M) using human lung adenocarcinoma A549. Also shown to reduce A549 cellular active Rac1 population (50 µ,M, 16 h) in vitro and effectively decrease liver tautomerase activity by 50% in mice (1 mg/animal/day or ~50 mg/kg/day via i.p.) in vivo., A cell-permeable iodo-pyrimidine compound that covalently modifies MIF N-terminal proline and exhibits higher MIF inhibitory potency than ISO-1 (Cat. No. 475837) in cell-free dopachrome tautomerase activity assays (IC50 ~5 vs. 50 µ,M, respectively, using recombinant human MIF) as well as in cell-based migration assays (50% vs 0% inhibition with respective inhibitor at 10 µ,M) and anchorage-independent growth (57% vs 0% inhibition with respective inhibitor at 10 µ,M) using human lung adenocarcinoma A549. Also shown to reduce A549 cellular active Rac1 population (50 µ,M, 16 h) in vitro and effectively decrease liver tautomerase activity by 50% in mice (1 mg/animal/day or ~50 mg/kg/day via i.p.) in vivo.