NAV-2729

SKU: orb1302055

Description

NAV-2729 is a potent small molecule inhibitor targeting multiple ArfGEFs, including human ARNO, EFA6, BIG1, and BRAG2, as well as bacterial RalF proteins. It demonstrates particularly strong activity against BRAG2, Arf1, and Arf6. This tool compound is valuable for in vitro studies investigating Arf GTPase signaling pathways in cancer and infectious disease research.

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 419547-11-8
• MW: 456.88
• Purity: 99.57% (May vary between batches)
• Formula: C₂₅H₁₇ClN₄O₃
• SMILES: [O-][N+](=O)c1ccc(cc1)-c1cc(=O)n2nc(Cc3ccccc3)c(-c3ccc(Cl)cc3)c2[nH]1
• Target: Others,Ras,GTPase
• Solubility: DMSO:6.88 mg/mL (15.06 mM)

Bioactivity

• In Vivo:
  In orthotopic xenograft mouse model of uveal melanoma, systemic treatment of NAV-2729 interfere with tumorigenesis and tumor growth.
• 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. 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. NAV-2729 is more effective toward Arf1 than Arf6.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NAV2729, NAV-2729, NAV 2729, Inhibitor, inhibit, Arf1, Arf6

Compound Identifiers

PubChem CID

2257249