Description: GI254023X is a potent MMP9 and ADAM10 inhibitor (IC50s: 2.5 and 5.3 nM) with 100-fold selectivity for the alpha-secretase ADAM10 over ADAM17 (TACE). GI254023X can remarkably inhibit the proliferation and induce the apoptosis of H929 cells, potentially through inhibition of Notch1 activation. Target:...

GI 254023X is an inhibitor of the metalloproteinase-disintegrin ADAM10 (IC50 = 5.3 nM). It is selective for ADAM10 over ADAM17, matrix metalloproteinase-1 (MMP-1), and MMP-3 (IC50s = 541, 108, and 187 nM, respectively), but also inhibits MMP-9 and MMP-13 (IC50s = 2.5 and 1.1 nM, respectively). GI 254023X inhibits...