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LY2510924

CAS No. : 1088715-84-7

MCE 站：LY2510924

产品活性：LY2510924是有效，选择性的 CXCR4 拮抗剂；阻止SDF-1结合CXCR4，IC₅₀值为0.079 nM。

研究领域：GPCR/G Protein  |  Immunology/Inflammation

作用靶点：CXCR

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

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

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