XL-784 is a selective inhibitor of matrix metalloproteinases (MMP). It shows IC50 values of approximately 1900, 0.81, 120, 10.8, 18, and 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9, and MMP-13, respectively. XL-784 is a highly potent, low-molecular-weight (1,122 g/mol) MMP inhibitor with limited aqueous solubility (20 μg/mL). It potently inhibits MMP-2, MMP-13, and ADAM10 [TNF-α-converting enzyme (TACE)] activity in vitro, with IC50 values in the range of 1-2 nM. XL-784 also inhibits MMP-9 (IC50 ~20 nM) and ADAM17 (IC50 ~70 nM) activity, but exhibits low potency for MMP-1 inhibition (IC50 ~2,000 nM). In vivo studies show that XL-784 is effective in inhibiting aortic dilatation in mice.
- Selective matrix metalloproteinases (MMP) inhibitor
- Potently inhibits MMP-2, MMP-13, and ADAM10 in vitro
- Inhibits MMP-9 and ADAM17 in vitro
- Effective in inhibiting aortic dilatation in vivo