Metalloproteinase inhibitors for the disintegrin-like metalloproteinases ADAM10 and ADAM17 that differentially block constitutive and phorbol ester-inducible shedding of cell surface molecules.

By A. Ludwig, C. Hundhausen, M. Lambert, N. Broadway, R. Andrews, D. Bickett, M. Leesnitzer, J. Becherer. 2005

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A Disintegrin and Metalloproteinase (ADAM) and ADAM with Thrombospondin Motifs (ADAMTS) Family in Vascular Biology and Disease (2019, background): “,Other inhibitors such as CGS27023, GW280264, and GI254023 exhibit specific inhibitory effect on ADAM-9, 10 and 17 [52].”
The ADAM metalloproteinases (2008, background): “This compound was used to provide evidence that ADAM-10 is involved in constitutive shedding of IL6R from cells, whereas PMA-stimulated shedding was inhibited by GW280264X, a mixed ADAM10/ADAM-17 inhibitor (Hundhausen et al., 2003; Ludwig et al., 2005) .”
Extracellular sphingomyelinase activity impairs TNF-α-induced endothelial cell death via ADAM17 activation and TNF receptor 1 shedding (2017, methodology): “1 U/ ml SMase for 3 hours in the presence or absence of the preferential ADAM10 inhibitor GI254023X (GI) and the ADAM10 and -17 inhibitor GW280264 (GW) [24].”
A Disintegrin and Metalloprotease (ADAM): Historical Overview of Their Functions (2016, background): “Other synthetic inhibitors include CGS 27023, GW280264, and GI254023 displaying a certain degree of specificity for ADAM-9, -10, and -17 [14,80].”