Gallein

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Cat.No. 3090 - Gallein | C20H12O7 | CAS No. 2103-64-2
Description: Inhibitor of βγ signaling
Chemical Name: 3',4',5',6'-Tetrahydroxyspiro[isobenzofuran-1(3H),9'-(9H)xanthen]-3-one
Purity: ≥97%
Datasheet
Citations (17)
Reviews (1)
Literature

Biological Activity

Inhibitor of G protein βγ subunit-dependent signaling. Blocks PI 3-kinase and Rac1 activation in HL60 cells and chemotaxis in HL60 differentiated cells.

Technical Data

M. Wt 364.31
Formula C20H12O7
Storage Store at -20°C
Purity ≥97%
CAS Number 2103-64-2
PubChem ID 73685
InChI Key PHLYOKFVXIVOJC-UHFFFAOYSA-N
Smiles OC1=CC=C(C(C(C=CC=C5)=C5C(O4)=O)4C(C=CC(O)=C3O)=C3O2)C2=C1O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 3.64 10
DMSO 27.32 75

Preparing Stock Solutions

The following data is based on the product molecular weight 364.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.74 mL 13.72 mL 27.45 mL
5 mM 0.55 mL 2.74 mL 5.49 mL
10 mM 0.27 mL 1.37 mL 2.74 mL
50 mM 0.05 mL 0.27 mL 0.55 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

Lehmann et al (2008) Small molecule disruption of G protein βγ subunit signaling inhibits neutrophil chemotaxis and inflammation. Mol.Pharmacol. 73 410 PMID: 18006643

Ukhanov et al (2011) Phosphoinositide 3-kinase-dependent antagonism in mammalian olfactory receptor neurons. J.Neurosci. 31 273 PMID: 21209212


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Keywords: Gallein, Gallein supplier, inhibitors, inhibits, betagamma, signaling, G, Proteins, Heterotrimeric, Protein, (Heterotrimeric), 3090, Tocris Bioscience

17 Citations for Gallein

Citations are publications that use Tocris products. Selected citations for Gallein include:

Chung et al (2015) Albumin-associated free fatty acids induce macropinocytosis in podocytes. J Clin Invest 125 2307 PMID: 25915582

Weber (2017) Activation of odorant receptor in colorectal cancer cells leads to inhibition of cell proliferation and apoptosis. PLoS One 12 e0172491 PMID: 28273117

Cameron (2017) Structural and pharmacological basis for the induction of mitochondrial biogenesis by formoterol but not clenbuterol. Sci Rep 7 10578 PMID: 28874749

Stott et al (2015) G-protein βγ subunits are positive regulators of Kv7.4 and native vascular Kv7 channel activity. Proc Natl Acad Sci U S A 112 6497 PMID: 25941381

López-Cotarelo et al (2015) A novel MEK-ERK-AMPK signaling axis controls chemokine receptor CCR7-dependent survival in human mature dendritic cells. Inflamm Res 290 827 PMID: 25425646

Sanz et al (2014) Promotion of cancer cell invasiveness and metastasis emergence caused by olfactory receptor stimulation. PLoS One 9 e85110 PMID: 24416348

Liu et al (2016) Activation of Adenosine 2A receptor inhibits neutrophil apoptosis in an autophagy-dependent manner in mice with systemic inflammatory response syndrome. Scientific Reports 6 33614 PMID: 27647162

Foster et al (2014) Bitter taste receptor agonists elicit G-protein-dependent negative inotropy in the murine heart. FASEB J 28 4497 PMID: 25002118

Gautam et al (2016) Tryptophan hydroxylase 1 and 5-HT7 receptor preferentially expressed in triple-negative breast cancer promote cancer progression through autocrine serotonin signaling. Mol Cancer 15 75 PMID: 27871326

Pon et al (2016) The β2-adrenoceptor activates a positive cAMP-calcium feedforward loop to drive breast cancer cell invasion. FASEB J 30 1144 PMID: 26578688

Breshears et al (2012) A disintegrin and metalloproteinase 17 (ADAM17) and epidermal growth factor receptor (EGFR) signaling drive the epithelial response to Staphylococcus aureus toxic shock syndrome toxin-1 (TSST-1). J Biol Chem 287 32578 PMID: 22833676

Salgado-Pabón et al (2013) Superantigens are critical for Staphylococcus aureus Infective endocarditis, sepsis, and acute kidney injury. MBio 4 PMID: 23963178

Ahmadiantehrani and Ron (2013) Dopamine D2 receptor activation leads to an up-regulation of glial cell line-derived neurotrophic factor via Gβγ-Erk1/2-dependent induction of Zif268. J Neurochem PMID: 23373701

Meens et al (2012) G-protein βγ subunits in vasorelaxing and anti-endothelinergic effects of calcitonin gene-related peptide. Br J Pharmacol 166 297 PMID: 22074193

Ukhanov et al (2011) Phosphoinositide 3-kinase-dependent antagonism in mammalian olfactory receptor neurons. J Neurosci 31 273 PMID: 21209212

Sikka et al (2014) Melanopsin mediates light-dependent relaxation in blood vessels. J Biol Chem 111 17977 PMID: 25404319

Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984 PMID: 21143600


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Reviews for Gallein

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Potent and reliable G protein beta gamma subunits
By Rocco Latorre on 12/13/2017
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: HEK 293 Cells

In-vivo (mouse) and in-vitro (HEK cells) experiments

Gallein is not easy to dissolve in solution, to do that is better dissolve gallein in a small quantity of DMSO and then reach your final concentration using Saline. Total DMSO% in the final volume should be no more then 0.5%.


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