MSX-122 is a small molecule and partial CXCR4 antagonist, directly binds to the CXCL12 site on CXCR4 and inhibits CXCR4/CXCL12 actions with IC50 of 10 nM.
MSX-122 (100 nM) effectively blocked invasion of 78% MDA-MB-231 cells while the same concentration of AMD3100 blocked invasion of 62% cells.
MSX-122 exhibits a different profile than AMD3100 and other reported anti-CXCR4 compounds: (1) MSX-122 did not inhibit T-tropic HIV infection (via the formation of the CXCR4/CD4/GP120 complex), while AMD3100; (2) unlike AMD3100, MSX-122 proved to be inactive in our calcium flux assay.
MSX-122 attenuates colonic damage in mice with experimental colitis, inhibits inflammation induced by carrageenan and lung fibrosis induced by bleomycin.
MSX-122 blocks metastasis in an experimental animal model of breast cancer metastasis, also inhibit metastatic progression in an orthotopic mouse model of uveal melanoma micrometastasis.