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NAV-2729 

Cat. No.: HY-112473 Purity: >98.0%
Handling Instructions

NAV-2729 is a dual Arf1/Arf6 activation inhibitor.

For research use only. We do not sell to patients.

NAV-2729 Chemical Structure

NAV-2729 Chemical Structure

CAS No. : 419547-11-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 390 In-stock
Estimated Time of Arrival: December 31
100 mg USD 660 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

NAV-2729 is a dual Arf1/Arf6 activation inhibitor.

IC50 & Target

Arf6[1][2]
Arf1[2]

In Vitro

NAV-2729 directly binds to Arf6. Based on a structural homology model of the Arf6/Arf6-GEF complex, it is predicted that NAV-2729 associates with Arf6 at the Arf6 GEF-binding area, which is distinct from the guanine nucleotide-binding pocket of Arf6. NAV-2729 blocks ARNO- and GEP100-mediated guanine nucleotide exchange on Arf6. The treatment of uveal melanoma cells with NAV-2729 interferes with anchorage-independent growth of the cell[1]. NAV-2729 is a dual Arf1/Arf6 inhibitor and is more effective toward Arf1 than Arf6. NAV-2729 blocks spontaneous activation of Arf6 and its activation by cytohesins and BRAG. NAV-2729 is an inhibitor of the spontaneous activation of Arf6, and it also inhibits the activation of Arf6 by its GEFs, ARNO and BRAG2, in solution. The inhibitory profile of NAV-2729 is analyzed at a concentration of 25 μM, which is reported to result in almost total inhibition of spontaneous and GEF-stimulated Arf6 activation in vitro. Under the conditions used in assays, NAV-2729 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[2].

In Vivo

Systemic treatment of mice with NAV-2729 interfere with tumorigenesis and tumor growth in orthotopic xenograft mouse model of uveal melanoma[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1888 mL 10.9438 mL 21.8876 mL
5 mM 0.4378 mL 2.1888 mL 4.3775 mL
10 mM 0.2189 mL 1.0944 mL 2.1888 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

456.88

Formula

C₂₅H₁₇ClN₄O₃

CAS No.

419547-11-8

SMILES

O=C1C=C(C2=CC=C([N+]([O-])=O)C=C2)NC3=C(C4=CC=C(Cl)C=C4)C(CC5=CC=CC=C5)=NN13

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
NAV-2729
Cat. No.:
HY-112473
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NAV-2729

Cat. No.: HY-112473