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NAV-2729 inhibits six ArfGEFs (human ARNO, EFA6, BIG1, and BRAG2 and Legionella and Rickettsia RalF), the strongest effects being against BRAG2, Arf1 and Arf6.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $38 | In Stock | |
5 mg | $61 | In Stock | |
10 mg | $97 | In Stock | |
25 mg | $215 | In Stock | |
50 mg | $318 | In Stock | |
100 mg | $477 | In Stock | |
500 mg | $987 | In Stock | |
1 mL x 10 mM (in DMSO) | $68 | In Stock |
Description | NAV-2729 inhibits six ArfGEFs (human ARNO, EFA6, BIG1, and BRAG2 and Legionella and Rickettsia RalF), the strongest effects being against BRAG2, Arf1 and Arf6. |
In vitro | 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]. |
In vivo | In orthotopic xenograft mouse model of uveal melanoma, systemic treatment of NAV-2729 interfere with tumorigenesis and tumor growth[2]. |
Molecular Weight | 456.88 |
Formula | C25H17ClN4O3 |
Cas No. | 419547-11-8 |
Smiles | [O-][N+](=O)c1ccc(cc1)-c1cc(=O)n2nc(Cc3ccccc3)c(-c3ccc(Cl)cc3)c2[nH]1 |
Relative Density. | 1.40 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 6.88 mg/mL (15.05 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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