BI-4394 is an inhibitor of matrix metalloproteinase-13 (MMP-13; IC50 = 0.001 ?M for the recombinant human enzyme).1 It is selective for MMP-13 over MMP-1-3, 7-10, -12, and -14 with IC50 values ranging from 8.3 to greater than 22 ?M for the recombinant human enzymes. BI-4394 inhibits the degradation of isolated bovine nasal cartilage explants cultured with human MMP-13 (IC50 = 0.031 ?M). It decreases disease severity in a mouse model of anti-type II collagen antibody and LPS-induced arthritis when administered at a dose of 100 mg/kg.2
1.Taylor, S.J., Abeywardane, A., Liang, S., et al.Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13J. Med. Chem.54(23)8174-8187(2011) 2.Taylor, S.J., Abeywardane, A., Liang, S., et al.Indole inhibitors of MMP-13 for arthritic disordersACS Omega6(29)18635-18650(2021)