Chemical Structure : FR900359
CAS No.:
107530-18-7
FR900359
(UBO-QIC)
Catalog No.: PC-22683Not For Human Use, Lab Use Only.
FR900359 is a plant-derived depsipeptide and specific pan-Gq (Gq/11/14) inhibitor, selectively inhibits Gq-dependent signalling, with little effect on Galphasbetagamma, Galphaibetagamma, or Galpha12/13betagamma heterotrimer activity.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
FR900359 is a plant-derived depsipeptide and specific pan-Gq (Gq/11/14) inhibitor, selectively inhibits Gq-dependent signalling, with little effect on Galphasbetagamma, Galphaibetagamma, or Galpha12/13betagamma heterotrimer activity.
FR900359 fully blocked Gq-mediated IP1 accumulation, did not perturb the cAMP-raising by Gs-sensitive prostanoid EP2/EP4 receptors or cAMP lowering by Gi-sensitive prostaglandin D2 receptor DP2/CRTH2.
FR900359 inhibits Gαq, Gα11 and Gα14, but not Gα16 or any other mammalian Gα isoform.
FR900359 does not impair G protein-independent β-arrestin recruitment. induces melanoma cells into differentiation and inhibits melanoma cell migration.
Physicochemical Properties
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M.Wt
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1002.17
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Formula
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C49H75N7O15
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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L-Threonine, (3R)-N-acetyl-3-hydroxy-L-leucyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-3-hydroxy-4-methyl-1-oxo-2-[(1-oxopropyl)amino]pentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone
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References
1. Schrage R, et al. Nat Commun. 2015 Dec 14;6:10156.
2. Carr R 3rd, et al. Mol Pharmacol. 2016 Jan;89(1):94-104.
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