FR900359 | pan-Gq inhibitor | Probechem Biochemicals

Chemical Structure : FR900359

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FR900359 (UBO-QIC)

货号: PC-22683Not For Human Use, Lab Use Only.

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生物&药学活性

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.

物理化学性质&存储条件

分子量	1002.17
分子式	C49H75N7O15
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

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.

FR900359 (UBO-QIC)

生物&药学活性

物理化学性质&存储条件

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FR900359 (UBO-QIC)

生物&药学活性

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