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 Ovalbumin, low endotoxin (HY-W250978A)-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

Solid

Light yellow to brown

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Room temperature in continental US; may vary elsewhere.

• [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]