2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. Grassofermata

Grassofermata is a dual Arf1/Arf6 activation inhibitor. ADP ribosylation factors (Arfs) are members of the Arf family of GTP-binding proteins of the Ras superfamily.

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

CAS No. : 419547-11-8

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Based on 11 publication(s) in Google Scholar

Grassofermata Related Antibodies

Top Publications Citing Use of Products

    Grassofermata purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2025 Jun 20;25(1):218.  [Abstract]

    Grassofermata (NAV-2729) (15 µM; 48 h) induced cell cycle arrest by inhibiting ARF6 in AML cell lines.

    Grassofermata purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2025 Jun 20;25(1):218.  [Abstract]

    Grassofermata (NAV-2729) (15 µM; 48 h) promoted apoptosis by inhibiting ARF6 in AML cell lines.

    Grassofermata purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2025 Jun 20;25(1):218.  [Abstract]

    ARF6 inhibitor (Grassofermata (NAV-2729)) (15 μmol/l; 48 h) regulated the PI3K/AKT/NF-κB signaling pathway to suppressed the proliferation and induced apoptosis in AML cells. (A) Expression of BCL-2 decreased and expression of P53 and BAX increased with NAV-2729. (B) Expression of CCND1 and C-MYC decreased and P21 increased with NAV-2729. (C) The levels of PI3K/AKT/NF-κB signaling pathway-related proteins were altered by NAV-2729 treatment (n=3 in each group).

    Grassofermata purchased from MedChemExpress. Usage Cited in: ACS Nano. 2024 Feb 27;18(8):6463-6476.  [Abstract]

    Cellular uptake of gold nanoparticles functionalized with different types of PEGs. In this case, the activity of Arf6, Cdc42, Endophilin A1, Caveolin, and Clathrin was respectively blocked with Grassofermata (NAV-2729) (20 μM, 2 h), CID44216842 (0.5 μM, 2 h), shRNA, PitoStop2 (10 μM, 2 h), and WL-47 (0.8 μM, 1 h) prior to the coculture with nanoparticles.

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    • References

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    Description

    Grassofermata is a dual Arf1/Arf6 activation inhibitor. ADP ribosylation factors (Arfs) are members of the Arf family of GTP-binding proteins of the Ras superfamily.

    IC50 & Target

    Arf6[1][2]
    Arf1[2]
    Cellular Effect
    Cell Line Type Value Description References
    HepG2 IC50
    6.3 μM
    Compound: Grassofermata; CB5
    Inhibition of FATP2 in human HepG2 cells assessed as decrease in fatty acid transport after 5 mins by trypan blue dye based fluorescence quenching method
    Inhibition of FATP2 in human HepG2 cells assessed as decrease in fatty acid transport after 5 mins by trypan blue dye based fluorescence quenching method
    		[PMID: 27446528]
    In Vitro

    Grassofermata directly binds to Arf6. Based on a structural homology model of the Arf6/Arf6-GEF complex, it is predicted that Grassofermata associates with Arf6 at the Arf6 GEF-binding area, which is distinct from the guanine nucleotide-binding pocket of Arf6. Grassofermata blocks ARNO- and GEP100-mediated guanine nucleotide exchange on Arf6. The treatment of uveal melanoma cells with Grassofermata interferes with anchorage-independent growth of the cell[1]. Grassofermata is a dual Arf1/Arf6 inhibitor and is more effective toward Arf1 than Arf6. Grassofermata blocks spontaneous activation of Arf6 and its activation by cytohesins and BRAG. Grassofermata 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 Grassofermata 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, Grassofermata inhibits spontaneous nucleotide exchange of Δ13Arf6 by ~15%. Grassofermata inhibits the activation of Δ13Arf6 by BRAG2Sec7PH by 25%. Δ17Arf1 has no measurable spontaneous nucleotide exchange. Activation of Δ17Arf1 by BRAG2Sec7PH is inhibited by Grassofermata, 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 Grassofermata for Δ17Arf1 while 50% inhibition is not achieved even at 25 μM Grassofermata for Δ13Arf6[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Grassofermata Related Antibodies
    In Vivo

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

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    456.88

    Formula

    C25H17ClN4O3
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (109.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.55 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.10%

    SDS (393 KB)

    COA (253 KB) HNMR (267 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1888 mL 10.9438 mL 21.8876 mL 54.7190 mL
    5 mM 0.4378 mL 2.1888 mL 4.3775 mL 10.9438 mL
    10 mM 0.2189 mL 1.0944 mL 2.1888 mL 5.4719 mL
    15 mM 0.1459 mL 0.7296 mL 1.4592 mL 3.6479 mL
    20 mM 0.1094 mL 0.5472 mL 1.0944 mL 2.7359 mL
    25 mM 0.0876 mL 0.4378 mL 0.8755 mL 2.1888 mL
    30 mM 0.0730 mL 0.3648 mL 0.7296 mL 1.8240 mL
    40 mM 0.0547 mL 0.2736 mL 0.5472 mL 1.3680 mL
    50 mM 0.0438 mL 0.2189 mL 0.4378 mL 1.0944 mL
    60 mM 0.0365 mL 0.1824 mL 0.3648 mL 0.9120 mL
    80 mM 0.0274 mL 0.1368 mL 0.2736 mL 0.6840 mL
    100 mM 0.0219 mL 0.1094 mL 0.2189 mL 0.5472 mL
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    Grassofermata Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Grassofermata419547-11-8NAV-2729NAV2729NAV 2729RasInhibitorinhibitorinhibit

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