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NAV-2729（Grassofermata）

  Cat. No.:  DC11971   Featured
Chemical Structure
419547-11-8
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More than 5000 active chemicals with high quality for research!
Field of application
NAV 2729 (NAV2729) is a chemical potentiator for mRNA-LNPs, increasing the delivery efficiencies of mRNA-LNPs in vitro and in vivo. NAV 2729 (NAV2729) is a novel, direct and selective small molecule inhibitor of small GTPase ARF6 with IC50 of 1.5 uM in nucleotide exchange assays.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 419547-11-8
Chemical Name: 2-benzyl-3-(4-chlorophenyl)-5-(4-nitrophenyl)pyrazolo[1,5-a]pyrimidin-7(4H)-one
Synonyms: NAV-2729;NAV2729
SMILES: C12=C(C3=CC=C(Cl)C=C3)C(CC3=CC=CC=C3)=NN1C(=O)C=C(C1=CC=C([N+]([O-])=O)C=C1)N2
Formula: C25H17ClN4O3
M.Wt: 456.88
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1. Yoo JH, et al. Cancer Cell. 2016 Jun 13;29(6):889-904. 2. Benabdi S, et al. Biochemistry. 2017 Sep 26;56(38):5125-5133.
Description: NAV-2729 is a dual Arf1/Arf6 activation inhibitor.
In Vivo: Systemic treatment of mice with NAV-2729 interfere with tumorigenesis and tumor growth in orthotopic xenograft mouse model of uveal melanoma[1].
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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DC11971 NAV-2729（Grassofermata） NAV 2729 (NAV2729) is a chemical potentiator for mRNA-LNPs, increasing the delivery efficiencies of mRNA-LNPs in vitro and in vivo. NAV 2729 (NAV2729) is a novel, direct and selective small molecule inhibitor of small GTPase ARF6 with IC50 of 1.5 uM in nucleotide exchange assays.
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