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NAV-2729

Catalog No. T5142 CAS 419547-11-8

NAV-2729 inhibits six ArfGEFs (human ARNO, EFA6, BIG1, and BRAG2 and Legionella and Rickettsia RalF), the strongest effects being against BRAG2, Arf1 and Arf6.

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NAV-2729, CAS 419547-11-8

Pack Size	Availability	Price/USD
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 215.00
50 mg	In stock	$ 318.00
100 mg	In stock	$ 477.00
500 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

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Purity: 98.83%

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Description	NAV-2729 inhibits six ArfGEFs (human ARNO, EFA6, BIG1, and BRAG2 and Legionella and Rickettsia RalF), the strongest effects being against BRAG2, Arf1 and Arf6.
In vitro	NAV-2729(25 μM) 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[1]. NAV-2729 blocks ARNO- and GEP100-mediated guanine nucleotide exchange on Arf6 and spontaneous activation of Arf6 and its activation by cytohesins and BRAG. The treatment of uveal melanoma cells with NAV-2729 interferes with anchorage-independent growth of the cell[1]. NAV-2729 is more effective toward Arf1 than Arf6[1].
In vivo	In orthotopic xenograft mouse model of uveal melanoma, systemic treatment of NAV-2729 interfere with tumorigenesis and tumor growth[2].

Molecular Weight	456.88
Formula	C25H17ClN4O3
CAS No.	419547-11-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (109.44 mM)

References and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library

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CCG-63808 RBC10 BQU57 CID-4785700 RBC8 QS11 ML-097 CCG-63802

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

NAV-2729 419547-11-8 GPCR/G Protein Others GTPase Inhibitor NAV 2729 inhibit NAV2729 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.