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Submit ReviewNAV 2729 is a selective ARF6 inhibitor (IC50 = 1.0 μM). Selective for ARF6 over other ARF family members and small GTPases. Inhibits ARF6 activation in uveal melanoma cells in vitro and blocks downstream signaling pathways of oncogenic GNAQ. Reduces tumorigenesis in mouse model of uveal melanoma.
NAV 2729 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 456.88 |
Formula | C25H17ClN4O3 |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 419547-11-8 |
PubChem ID | 2257249 |
InChI Key | WHYGBVWGARJOCS-UHFFFAOYSA-N |
Smiles | ClC1=CC=C(C2=C3NC(C4=CC=C([N+]([O-])=O)C=C4)=CC(N3N=C2CC5=CC=CC=C5)=O)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 45.69 | 100 |
The following data is based on the product molecular weight 456.88. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.19 mL | 10.94 mL | 21.89 mL |
5 mM | 0.44 mL | 2.19 mL | 4.38 mL |
10 mM | 0.22 mL | 1.09 mL | 2.19 mL |
50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
References are publications that support the biological activity of the product.
Yoo et al (2016) ARF6 is an actionable node that orchestrates oncogenic GNAQ signaling in uveal melanoma. Cancer Cell. 29 889 PMID: 27265506
If you know of a relevant reference for NAV 2729, please let us know.
Keywords: NAV 2729, NAV 2729 supplier, NAV2729, small, G, proteins, Gαq, GTPases, inhibitors, inhibits, selective, ARF6, GNAQ, Arf, 5986, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for NAV 2729 include:
Gavin Y et al (2019) Bone Marrow-Derived Cells Restore Functional Integrity of the Gut Epithelial and Vascular Barriers in a Model of Diabetes and ACE2 Deficiency. Circ Res 125 969-988 PMID: 31610731
Finicle et al (2018) Sphingolipids inhibit endosomal recycling of nutrient transporters by inactivating ARF6. J Cell Sci 131 PMID: 29848659
Renate et al (2022) Pharmacological Inhibition of Lipid Import and Transport Proteins in Ovarian Cancer. Cancers (Basel) 14 PMID: 36497485
Karlheinz et al (2020) Complement C5a Induces Pro-inflammatory Microvesicle Shedding in Severely Injured Patients. Front Immunol 11 1789 PMID: 32983087
Ernst et al (2019) Humanized anti-CD123 antibody facilitates NK cell antibody-dependent cell-mediated cytotoxicity (ADCC) of Hodgkin lymphoma targets via ARF6/PLD-1. Blood Cancer J 9 6 PMID: 30647406
Do you know of a great paper that uses NAV 2729 from Tocris? Please let us know.
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