NAV 2729
Chemical Name: 3-(4-Chlorophenyl)-5-(4-nitrophenyl)-2-(phenylmethyl)pyrazolo[1,5-a]pyrimidin-7(4H)-one
Purity: ≥98%
Biological Activity
NAV 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.Technical Data
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.
Background References
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ARF6 is an actionable node that orchestrates oncogenic GNAQ signaling in uveal melanoma.
Yoo et al.
Cancer Cell., 2016;29:889 -
Simultaneous inhibition of endocytic recycling and lysosomal fusion sensitizes cells and tissues to oligonucleotide therapeutics
BT Finicle, KH Eckenstein, AS Revenko, BA Anderson, WB Wan, AN McCracken, D Gil, DA Fruman, S Hanessian, PP Seth, AL Edinger
Nucleic Acids Research, 2023;0(0):.
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Citations for NAV 2729
The citations listed below are publications that use Tocris products. Selected citations for NAV 2729 include:
5 Citations: Showing 1 - 5
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Pharmacological Inhibition of Lipid Import and Transport Proteins in Ovarian Cancer.
Authors: Renate Et al.
Cancers (Basel) 2022;14
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Complement C5a Induces Pro-inflammatory Microvesicle Shedding in Severely Injured Patients.
Authors: Karlheinz Et al.
Front Immunol 2020;11:1789
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Humanized anti-CD123 antibody facilitates NK cell antibody-dependent cell-mediated cytotoxicity (ADCC) of Hodgkin lymphoma targets via ARF6/PLD-1.
Authors: Ernst Et al.
Blood Cancer J 2019;9:6
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Bone Marrow-Derived Cells Restore Functional Integrity of the Gut Epithelial and Vascular Barriers in a Model of Diabetes and ACE2 Deficiency.
Authors: Gavin Y Et al.
Circ Res 2019;125:969-988
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Sphingolipids inhibit endosomal recycling of nutrient transporters by inactivating ARF6.
Authors: Finicle Et al.
J Cell Sci 2018;131
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