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NAV2729 (Synonyms: NAV2729)

Catalog No.GC18523

Grassofermata is an inhibitor of fatty acid transport.

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NAV2729 Chemical Structure

Cas No.: 419547-11-8

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1mg
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5mg
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10mg
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25mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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

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].

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

References:
[1]. Yamauchi Y, et al. Machineries regulating the activity of the small GTPase Arf6 in cancer cells are potential targets for developing innovative anti-cancer drugs. Adv Biol Regul. 2017 Jan;63:115-121.
[2]. Benabdi S, et al. Family-wide Analysis of the Inhibition of Arf Guanine Nucleotide Exchange Factors with Small Molecules: Evidence of Unique Inhibitory Profiles. Biochemistry. 2017 Sep 26;56(38):5125-5133.

Chemical Properties

Cas No. 419547-11-8 SDF
Synonyms NAV2729
Chemical Name 3-(4-chlorophenyl)-5-(4-nitrophenyl)-2-(phenylmethyl)-pyrazolo[1,5-a]pyrimidin-7(4H)-one
Canonical SMILES O=C(C=C(C1=CC=C([N+]([O-])=O)C=C1)N2)N3C2=C(C4=CC=C(Cl)C=C4)C(CC5=CC=CC=C5)=N3
Formula C25H17ClN4O3 M.Wt 456.9
Solubility DMSO: 2 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.1887 mL 10.9433 mL 21.8866 mL
5 mM 0.4377 mL 2.1887 mL 4.3773 mL
10 mM 0.2189 mL 1.0943 mL 2.1887 mL
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

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