CWHM12 is a pan αv integrin antagonist [1
]. It was used to determine that αv integrin activation regulates fibrosis in models of organ fibrosis. These findings suggest that targeting all αv integrins may have clinical utility in the treatment of a broad range of fibrotic diseases. The S
enantiomer of CWHM12 is the bioactive form; the R
enantiomer does not inhibit any of the five αv-containing integrins in vitro
Structurally, CWHM12 is a small-molecule RGD peptidomimetic antagonist in which the arginine (R) mimetic is a cyclic guanidino-substituted phenyl group and the aspartic acid (D) mimetic is a phenyl-substituted β amino acid. These two residues are linked by a glycine (G).