PAI-1-IN-1 is an orally active and specific PAI-1 inhibitor with an IC 50 of <6.95 μM. PAI-1-IN-1 blocks the interaction between PAI-1 and serine proteases or LRP-1 , and enhances plasmin generation. PAI-1-IN-1 restores macrophage efferocytosis and promotes macrophage polarization. PAI-1-IN-1 alleviates PAI-1 -mediated inhibition of Furin , promotes MT1-MMP maturation, activates the NOTCH1 signaling pathway, inhibits proliferation and induces apoptosis . PAI-1-IN-1 promotes skeletal muscle regeneration and alleviates inflammation in a mouse model of skeletal muscle injury. PAI-1-IN-1 can be used in research on skeletal muscle injury-induced inflammation and chronic myeloid leukemia.
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