LY2510924 is an effective and selective CXCR4 antagonist. It blocks SDF-1 binding to CXCR4 (IC50: 0.079 nM).

SDF-1α-CXCR4:49.5 pM (ki), SDF-1α-CXCR4:79.7 pM

LY2510924 inhibits SDF-1–induced cell migration (IC50: 0.26 nM) and inhibits SDF-1/CXCR4-mediated intracellular signaling, in human lymphoma U937 cells expressing endogenous CXCR4. LY2510924 also inhibits SDF-1–induced GTP binding (Kb: 0.38 nM). LY2510924 specifically blocks SDF-1 binding to CXCR4 (IC50: 0.079 nM). LY2510924 displays a concentration-dependent inhibition of SDF-1–stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveal that LY2510924 has no apparent agonist activity[1]. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells[2].