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NAV-2729

🥰Excellent
Catalog No. T5142Cas No. 419547-11-8

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.

NAV-2729

NAV-2729

🥰Excellent
Purity: 98.91%
Catalog No. T5142Cas No. 419547-11-8
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 SizePriceAvailabilityQuantity
2 mg$38In Stock
5 mg$61In Stock
10 mg$97In Stock
25 mg$215In Stock
50 mg$318In Stock
100 mg$477In Stock
500 mg$987In Stock
1 mL x 10 mM (in DMSO)$68In Stock
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Purity:98.91%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight456.88
FormulaC25H17ClN4O3
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 & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.1888 mL10.9438 mL21.8876 mL109.4379 mL
5 mM0.4378 mL2.1888 mL4.3775 mL21.8876 mL
10 mM0.2189 mL1.0944 mL2.1888 mL10.9438 mL

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