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NAV-2729

CAS No. : 419547-11-8

MCE 站：NAV-2729

产品活性：NAV-2729 是一种 Arf1/Arf6 活化抑制剂。

研究领域：Others

作用靶点：Others

In Vitro: NAV-2729 directly binds to Arf6. Based on a structural homology model of the Arf6/Arf6-GEF complex, it is predicted that NAV-2729 associates with Arf6 at the Arf6 GEF-binding area, which is distinct from the guanine nucleotide-binding pocket of Arf6. NAV-2729 blocks ARNO- ａnd GEP100-mediated guanine nucleotide exchange on Arf6. The treatment of uveal melanoma cells with NAV-2729 interferes with anchorage-independent growth of the cell. NAV-2729 is a dual Arf1/Arf6 inhibitor ａnd is more effective toward Arf1 than Arf6. NAV-2729 blocks spontaneous activation of Arf6 ａnd its activation by cytohesins ａnd BRAG. NAV-2729 is an inhibitor of the spontaneous activation of Arf6, ａnd it also inhibits the activation of Arf6 by its GEFs, ARNO ａnd BRAG2, in solution. The inhibitory profile of NAV-2729 is analyzed at a concentration of 25 μM, which is reported to result in almost total inhibition of spontaneous ａnd GEF-stimulated Arf6 activation in vitro. Under the conditions used in assays, NAV-2729 inhibits spontaneous nucleotide exchange of Δ13Arf6 by ~15%. NAV-2729 inhibits the activation of Δ13Arf6 by BRAG2^Sec7PH by 25%. Δ17Arf1 has no measurable spontaneous nucleotide exchange. Activation of Δ17Arf1 by BRAG2^Sec7PH is inhibited by NAV-2729, ａnd the efficiency is markedly higher than that for Arf6 (50%). In a dose-response experiment, nucleotide exchange rates are reduced by 50% by 10 μM NAV-2729 for Δ17Arf1 while 50% inhibition is not achieved even at 25 μM NAV-2729 for Δ13Arf6.

In Vivo: Systemic treatment of mice with NAV-2729 interfere with tumorigenesis ａnd tumor growth in orthotopic xenograft mouse model of uveal melanoma.

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