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Submit ReviewGallein
Description: Inhibitor of Gβ/γ signaling
Chemical Name: 3',4',5',6'-Tetrahydroxyspiro[isobenzofuran-1(3H),9'-(9H)xanthen]-3-one
Purity: ≥97%
Biological Activity for Gallein
Gallein is an 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 for Gallein
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Gallein
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.32 | 75 | |
| ethanol | 3.64 | 10 |
Preparing Stock Solutions for Gallein
The following data is based on the product molecular weight 364.31. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.75 mM | 3.66 mL | 18.3 mL | 36.6 mL |
| 3.75 mM | 0.73 mL | 3.66 mL | 7.32 mL |
| 7.5 mM | 0.37 mL | 1.83 mL | 3.66 mL |
| 37.5 mM | 0.07 mL | 0.37 mL | 0.73 mL |
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Product Datasheets for Gallein
References for Gallein
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, G-protein, GTPases, 3090, Tocris Bioscience
21 Citations for Gallein
Citations are publications that use Tocris products. Selected citations for Gallein include:
Travers et al (2017) Pharmacological and Activated Fibroblast Targeting of Gβγ-GRK2 After Myocardial Ischemia Attenuates Heart Failure Progression. J Am Coll Cardiol 70 958 PMID: 28818206
Xiao et al (2017) Biased OXTergic Modulation of Midbrain DA Systems. Neuron 95 368 PMID: 28669546
Chung et al (2015) Albumin-associated free fatty acids induce macropinocytosis in podocytes. J Clin Invest 125 2307 PMID: 25915582
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
Cervantes-Villagrana et al (2019) Protumoral bone marrow-derived cells migrate via Gβγ-dependent signaling pathways and exhibit a complex repertoire of RhoGEFs. J Cell Commun Signal 13 179 PMID: 30612298
Cameron (2017) Structural and pharmacological basis for the induction of mitochondrial biogenesis by formo. but not clenbu. Sci Rep 7 10578 PMID: 28874749
Ukhanov et al (2011) Phosphoinositide 3-kinase-dependent antagonism in mammalian olfactory receptor neurons. J Neurosci 31 273 PMID: 21209212
Weber (2017) Activation of odorant receptor in colorectal cancer cells leads to inhibition of cell proliferation and apoptosis. PLoS One 12 e0172491 PMID: 28273117
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) DA 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
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
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
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
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
Foster et al (2014) Bitter taste receptor agonists elicit G-protein-dependent negative inotropy in the murine heart. FASEB J 28 4497 PMID: 25002118
Zhao et al (2018) Ethanolic Extract of Folium Sennae Mediates the Glucose Uptake of L6 Cells by GLUT4 and Ca2. Molecules 23 PMID: 30424024
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Reviews for Gallein
Average Rating: 4 (Based on 1 Review.)
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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%.