| Bioactivity | FR900359 is a depsipeptide selective inhibitor of Gαq/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]. |
| Invitro | FR900359 (1.0 μM，1 小时) 在 HEK293 细胞中抑制 Gαq、Gα11 和 Gα/14，但不抑制 Gα<16 或任何其他哺乳动物 Gα 亚型[1]。FR900359 (0-10 μM, 24 小时) 以浓度依赖的方式有效地减少 B16 细胞的生长，抑制增殖及迁移[1]。FR900359 (10 nM, 72 小时) 诱导黑色素瘤细胞 G1 细胞周期停滞，使其分化[1]。FR900359 (1.0 μM, 5 分钟) 阻断 Gq 依赖性 ERK1/2 激活[1]。FR900359 (1 μM, 24 小时) 与未处理组相比，显著诱导更多的 92.1 细胞发生凋亡[3]。FR900359 (30 nM，60 分钟) 诱导小鼠、猪和人体外气道发生剂量依赖性松弛[4]。 Cell Proliferation Assay[1] Cell Line: |
| In Vivo | FR900359 (0.2 或1 mg/ml, 每只鼠 12 μL, 静脉注射) 显著降低小鼠尾静脉血管张力[1]。FR900359 (0.1 mg/ml，2.5 mg/小鼠，气管内给药) 消除了 Ovalbumin (HY-W250978) 诱导的小鼠致敏后的气道高反应性[4]。 Animal Model: |
| Name | FR900359 |
| CAS | 107530-18-7 |
| Formula | C49H75N7O15 |
| Molar Mass | 1002.16 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Schrage R, et.al. The experimental power of FR900359 to study Gq-regulated biological processes. Nat Commun. 2015 Dec 14;6:10156. [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. [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. |