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EHop-016

CAS No. : 1380432-32-5

MCE 站：EHop-016

产品活性：EHop-016 是一种有效的选择性的 Rac GTPase Rac1 和 Rac3 抑制剂。EHop-016 在 MDA-MB-435 细胞中抑制 Rac1 活性，IC₅₀ 为 1.1 μM。EHop-016 抑制 Vav2 与 Rac，Rac 激活的 PAK1 相互作用，片状脂蛋白形成和细胞迁移。

研究领域：GPCR/G Protein

作用靶点：Ras

In Vitro: EHop-016 (1-10 μM; 24 hours; MDA-MB-435 cells) treatment inhibits Rac1 and Rac3 activity. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells that demonstrate high active levels of the Rac GEF Vav2, EHop-016 inhibits the association of Vav2 with a nucleotide-free Rac1(G15A) .
EHop-016 also inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation in both cell lines. EHop-016 decreases Rac downstream effects of PAK1 (p21-activated kinase 1) activity and directed migration of metastatic cancer cells.
EHop-016 affectes cell viability by down-regulating Akt and Jun kinase activities and c-Myc and Cyclin D expression, as well as increasing caspase 3/7 activities in metastatic cancer cells.

In Vivo: EHop-016 (10-25 mg/kg; intraperitoneal injection; 3 times a week; for 55 days; nu/nu mice) treatment significantly reduces mammary fat pad tumor growth, metastasis, and angiogenesis.

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