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]. In Vitro: 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].
In Vivo: 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].