Here, we reported the beneficial effects of DUSP6 allosteric inhibitor BCI, by improving cardiac function and ameliorating cardiac inflammation and fibrosis at least partly through attenuating p38–NF-κB signaling, and local delivery of a single dose of PLGA-encapsulated BCI had notable effects on cardiac repair post-MI. The gene discussed is DUSP6; the disease is myocardial infarction.