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Gallein

Catalog No.
B7271
Inhibitor of G protein βγ subunit-dependent signaling
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$50.00
In stock
50mg
$103.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

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Email: [email protected]

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Background

Gallein is a small inhibitor of G protein βγ (Gβγ) subunit signalling [1]. 

Gβγ subunits are central participants in G protein-coupled receptor (GPCR) signaling pathways. Gβγ subunits interact with receptors, G protein α subunits and downstream targets to coordinate multiple, different GPCR functions [2]. 

In spheroids made by LNCaP cells and grown in collagen gels, gallein at 10 µM was able to significantly counteract β-ionone-induced LNCaP cell invasiveness [1]. In human monocyte-derived macrophages, gallein effectively inhibited M1 polarization and promoted M2 polarization [3]. 

In castrated male NSG mice carrying subcutaneous injected LNCaP cells, intraperitoneal injection of gallein (5 mg/kg/day) inhibited β-ionone-mediated metastasis spread [1]. In a rat model of autoimmune myocarditis, gallein (10 mg/kg/day, p.o., for 21 days) effectively improved survival and cardiac function, suppressed cardiac remodeling, and further attenuated myocardial protein expression of G protein-coupled receptor kinase 2 (GRK2) as well as high mobility group box 1 (HMGB1) and its cascade signaling proteins [3]. 

References:

[1]. Sanz G, Leray I, Muscat A, et al. Gallein, a Gβγ subunit signalling inhibitor, inhibits metastatic spread of tumour cells expressing OR51E2 and exposed to its odorant ligand. BMC Research Notes, 2017, 10(1): 541.

[2]. Smrcka A V. G protein βγ subunits: central mediators of G protein-coupled receptor signaling. Cellular and Molecular Life Sciences, 2008, 65(14): 2191-2214.

[3]. Karuppagounder V, Bajpai A, Meng S, et al. Small molecule disruption of G protein βγ subunit signaling reprograms human macrophage phenotype and prevents autoimmune myocarditis in rats. PLoS One, 2018, 13(7): e0200697.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt364.31
Cas No.2103-64-2
FormulaC20H12O7
Solubilityinsoluble in EtOH; insoluble in H2O; ≥18.1 mg/mL in DMSO
Chemical Name3',4',5',6'-tetrahydroxy-3H-spiro[isobenzofuran-1,9'-xanthen]-3-one
SDFDownload SDF
Canonical SMILESO=C1O[C@]2(C(C=CC(O)=C3O)=C3OC4=C2C=CC(O)=C4O)C5=CC=CC=C51
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

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