FR900359 

FR900359 is a depsipeptide selective inhibitor of Gα_q/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumins(HY-W250978)–induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research^[1][2][3][4].

FR900359 (1.0 μM, 1 hours) inhibits Gα_q, Gα₁₁ and Gα _/14, but not Gα₁₆ or any other mammalian Gα isoform in HEK293 cells^[1].
FR900359 (0-10 μM, 24 hours) effectively reduces growth of B16 cells and suppressed cell proliferation and inhibits migration in a concentration-dependent manner^[1].
FR900359 (10 nM, 72 hours) induces G1 cell cycle arrest in melanoma cells with Gq tone and forces melanoma cells (B16 cells) into differentiation ^[1].
FR900359 (1.0 μM, 5 min) interdicts the activation of extracellular signal-regulated kinases 1 and 2 (ERK1/2) that be largely Gq-mediated28^[1].
FR900359 (1 μM, 24 hours) significantly induces more 92.1 cells undergoing apoptosis compared to untreated ^[3].
FR900359 (30 nM, 60 min) induces dose-dependent relaxation of murine, porcine, and human airways ex vivo^[4].

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

FR900359 (0.2 or 1 mg/ml, 12 μL per mouse, i.v.) strongly reduces vascular tone in mouse tail artery^[1].
FR900359 (0.1 mg/ml, 2.5 mg/mouse, intratracheally) abolishes airway hyperreactivity after Ovalbumin (HY-W250978)-induced sensitization in mice^[4].

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

1002.16

C₄₉H₇₅N₇O₁₅

107530-18-7

Liquid

Colorless to light yellow

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Room temperature in continental US; may vary elsewhere.

Solution, -20°C, 2 years

• [1]. Schrage R, et.al. The experimental power of FR900359 to study Gq-regulated biological processes. Nat Commun. 2015 Dec 14;6:10156.  [Content Brief]

  [2]. Fujioka, M,et.al. Structure of FR900359, a cyclic depsipeptide from Ardisia crenata sims J. Org. Chem. 1988, 53 (12), 2820−2825.

  [3]. Lapadula D, et.al. Effects of Oncogenic Gαq and Gα11 Inhibition by FR900359 in Uveal Melanoma. Mol Cancer Res. 2019 Apr;17(4):963-973.  [Content Brief]

  [4]. Matthey M, et.al. Targeted inhibition of Gq signaling induces airway relaxation in mouse models of asthma. Sci Transl Med. 2017 Sep 13;9(407):eaag2288.  [Content Brief]