化合物NAV-2729 T5142

Product Introduction
Bioactivity


英文名: NAV-2729

描述: NAV-2729 是有效的Arf1/Arf6活化抑制剂。

体外活性: NAV-2729(25 μM) inhibits spontaneous nucleotide exchange of Δ13Arf6 by ~15%. NAV-2729 inhibits the activation of Δ13Arf6 by BRAG2Sec7PH by 25%. Δ17Arf1 has no measurable spontaneous nucleotide exchange. Activation of Δ17Arf1 by BRAG2Sec7PH 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[1]. NAV-2729 blocks ARNO- and GEP100-mediated guanine nucleotide exchange on Arf6 and spontaneous activation of Arf6 and its activation by cytohesins and BRAG. The treatment of uveal melanoma cells with NAV-2729 interferes with anchorage-independent growth of the cell[1]. NAV-2729 is more effective toward Arf1 than Arf6[1].

体内活性: In orthotopic xenograft mouse model of uveal melanoma, systemic treatment of NAV-2729 interfere with tumorigenesis and tumor growth[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 6.88 mg/mL (15.05 mM)


关键字: Inhibitor | NAV 2729 | inhibit | NAV2729 | NAV-2729

相关产品: Tyrphostin 8 | Gancaonin I | RBC8 | CCG-63802 | Compound C108 | IMM-01 | CID-4785700 | RBC10 | CCG-50014 | ML-097

相关库: Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | GPCR Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途