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ISO-1 is a small molecule inhibitor of macrophage migration inhibitory factor (MIF), specifically inhibiting its D-dopachrome tautomerase activity with an IC50 of approximately 7 μM[1][7]. It binds to the active site of MIF and blocks its biological activities, including pro-inflammatory signaling. ISO-1 has demonstrated protective effects in various preclinical models such as sepsis, diabetes mellitus, asthma (airway remodeling), and inflammatory/fibrotic lung disease[5][7]. It is cell-permeable and orally bioavailable. The compound has been shown to cross the blood-brain barrier and suppresses inflammatory responses in several animal models. Its primary mechanism is antagonism of MIF-mediated pathways involved in immune regulation and inflammation[5][6].
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