NAV-2729
{[allProObj[0].p_purity_real_show]}
货号：A691659
同义名：
Grassofermata
NAV-2729是选择性的 ARF6 抑制剂，IC50 为 1 μM。
NAV-2729 化学结构
NAV-2729 3D分子结构
规格
价格
会员价
库存
数量
{[ item.pr_size ]}
{[ getRatePriceInt(item.pr_rmb, 1,1) ]}
{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]}
{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}
{[ getRatePriceInt(item.pr_rmb, 1,1) ]}
{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]}
{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}
{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}
{[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]}
{[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]}
{[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]}
现货
1周
咨询
-
+
NAV-2729 纯度/质量文件 产品仅供科研
货号：A691659
标准纯度：
{[allProObj[0].p_purity_real_show]}
产品说明书
全球学术期刊中引用的产品
• Nature , 2025, 645, 793-800. Ambeed. A201204 ,
A444152 ,
A344107 ,
A952055
]
• Cell , 2025. Ambeed. A122167
]
• Science , 2025, 387(6729): eadp5637. Ambeed. • Sig. Transduct. Target. Ther. , 2025, 10, 257. Ambeed. A104916
]
• Nat. Nanotechnol. , 2025. Ambeed. A1216705 ,
A522597 ,
A125401 ,
A1355641
]
更多 >
NAV-2729 质控信息
NAV-2729 生物活性
描述
ARF6 (GTPase ADP-ribosylation factor 6) can be activated by a variety of different ARF-guanine nucleotide exchange factors (ARF-GEFs), depending on the stimulating factor or cell type and is an attractive candidate as an effector of Gαq signaling. NAV-2729 is allosteric, non-nucleotide-competitive and reversible ARF6-selective inhibitor with IC50 value of 1.5μM. NAV-2729 directly inhibited ARF6 as evidenced by nearly equipotent inhibitory effects toward spontaneous and ARF-GEF-catalyzed ARF6 nucleotide exchange. Treatment of Mel92.1 and Mel202 cells with NAV-2729 at concentration of 10μM inhibited ARF6 activation, as well as mimicked ARF6 and GEP100 knockdown by driving GNAQ from the cytoplasmic vesicles to the plasma membrane and reducing anchorage-independent colony growth. NAV-2729 also blocked all of the known downstream signaling pathways of oncogenic GNAQ, including PLC/PKC, Rho/Rac, YAP, and β-catenin. Administration of NAV-2729 at dose of 30mg/kg, i.p., daily, reduced uveal melanoma cell proliferation and tumorigenesis in a mouse model[2]
作用机制
NAV-2729 targets ARF6 GEF-binding region.[2]
NAV-2729 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Kidney organoids
10 µM
2 hours
NAV-2729 significantly reduced viral infection
J Gen Virol. 2023 Jun;104(6):001868
Calu-3 cells
10 µM
2 hours
NAV-2729 significantly reduced viral infection
J Gen Virol. 2023 Jun;104(6):001868
Huh-7 cells
10 µM
2 hours
NAV-2729 showed a dose-dependent inhibition of infection
J Gen Virol. 2023 Jun;104(6):001868
C2C12
11 ± 2 µM (EC50)
3 days
NAV-2729 inhibited C2C12 cell proliferation with an EC50 of 11 ± 2 μM.
J Biol Chem. 2023 Mar;299(3):102992
NIH 3T3
11 ± 3 µM (EC50)
3 days
NAV-2729 inhibited NIH 3T3 cell proliferation with an EC50 of 11 ± 3 μM.
J Biol Chem. 2023 Mar;299(3):102992
MCF 10A
10 ± 4 µM (EC50)
3 days
NAV-2729 inhibited MCF 10A cell proliferation with an EC50 of 10 ± 4 μM.
J Biol Chem. 2023 Mar;299(3):102992
HeLa
9 ± 2 µM (EC50)
3 days
NAV-2729 inhibited HeLa cell proliferation with an EC50 of 9 ± 2 μM.
J Biol Chem. 2023 Mar;299(3):102992
SMS-CTR
11 ± 5 µM (EC50)
3 days
NAV-2729 inhibited SMS-CTR cell proliferation with an EC50 of 11 ± 5 μM.
J Biol Chem. 2023 Mar;299(3):102992
RD
8 ± 4 µM (EC50)
3 days
NAV-2729 inhibited RD cell proliferation with an EC50 of 8 ± 4 μM.
J Biol Chem. 2023 Mar;299(3):102992
OSA
9 ± 2 µM (EC50)
3 days
NAV-2729 inhibited OSA cell proliferation with an EC50 of 9 ± 2 μM.
J Biol Chem. 2023 Mar;299(3):102992
U2OS
9 ± 1 µM (EC50)
3 days
NAV-2729 inhibited U2OS cell proliferation with an EC50 of 9 ± 1 μM.
J Biol Chem. 2023 Mar;299(3):102992
Pig coronary artery smooth muscle cells
5 µM
30 minutes
NAV2729 inhibited concentration-dependent contractions induced by carbachol and methacholine
Naunyn Schmiedebergs Arch Pharmacol. 2022 Apr;395(4):471-485
Pig interlobar artery smooth muscle cells
5 µM and 10 µM
30 minutes
NAV2729 inhibited frequency-dependent EFS-induced contractions
Naunyn Schmiedebergs Arch Pharmacol. 2022 Apr;395(4):471-485
展开
NAV-2729 动物研究
Dose
Mice: 30 mg/kg[2]
Administration
i.p.
NAV-2729 参考文献
[1] Yoo JH, Shi DS, et al. ARF6 Is an Actionable Node that Orchestrates Oncogenic GNAQ Signaling in Uveal Melanoma. Cancer Cell. 2016 Jun 13;29(6):889-904.
[2] Yoo JH, Shi DS, Grossmann AH, Sorensen LK, Tong Z, Mleynek TM, Rogers A, Zhu W, Richards JR, Winter JM, Zhu J, Dunn C, Bajji A, Shenderovich M, Mueller AL, Woodman SE, Harbour JW, Thomas KR, Odelberg SJ, Ostanin K, Li DY. ARF6 Is an Actionable Node that Orchestrates Oncogenic GNAQ Signaling in Uveal Melanoma. Cancer Cell. 2016 Jun 13;29(6):889-904. doi: 10.1016/j.ccell.2016.04.015. Epub 2016 Jun 2. PMID: 27265506; PMCID: PMC5027844.
NAV-2729 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.19mL
0.44mL
0.22mL
10.94mL
2.19mL
1.09mL
21.89mL
4.38mL
2.19mL
NAV-2729 技术信息
搜索
