| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Gallein targets G protein βγ subunits, which are key signaling molecules that mediate signaling from G protein-coupled receptors (GPCRs) to various downstream effectors. By binding to Gβ1γ2 with an IC50 of 200 nM, Gallein inhibits Gβγ-dependent signaling pathways, including the activation of PI3K. This inhibition can affect a range of cellular processes, including cell migration, proliferation, and survival. The compound's ability to inhibit Gβγ signaling makes it a valuable tool for studying GPCR signaling.
|
|---|---|
| ln Vitro |
Gallein binds to Gβ1γ2 in a cell-free assay with an IC50 of 200 nM. It inhibits Gβγ-dependent activation of PI3K in HL-60 cells. The compound has been shown to inhibit metastatic spread of tumor cells expressing OR51E2 when exposed to its odorant ligand. Gallein also exhibits anti-inflammatory, antioxidant, and anticancer properties. These activities make it a versatile tool for studying Gβγ signaling and its role in various biological processes.
|
| ln Vivo |
Gallein has been shown to inhibit metastatic spread of tumor cells expressing OR51E2 and exposed to its odorant ligand. This suggests potential for studying cancer metastasis and the role of GPCR signaling in tumor progression. Further research is needed to evaluate its efficacy in other in vivo models. The compound's ability to inhibit Gβγ signaling and its various biological activities make it a valuable tool for pharmacological research.
|
| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for Gallein typically involves a binding assay to measure its interaction with Gβ1γ2 subunits. Recombinant Gβ1γ2 protein is incubated with varying concentrations of Gallein, and binding is measured using fluorescence polarization, surface plasmon resonance (SPR), or other biophysical methods. Alternatively, a Gβγ-dependent signaling assay can be performed using purified components to measure the compound's ability to inhibit Gβγ-mediated activation of downstream effectors such as PI3K.
|
| Cell Assay |
The in vitro cellular assay for Gallein typically uses HL-60 cells or other cell lines to assess its effects on Gβγ-dependent signaling. Cells are treated with varying concentrations of Gallein, and Gβγ-dependent activation of PI3K is measured by assessing AKT phosphorylation or PIP3 production. The compound's effects on cell migration, proliferation, and apoptosis can be assessed using standard cell-based assays. In tumor cells expressing OR51E2, the effects on metastatic spread can be evaluated in migration and invasion assays.
|
| Animal Protocol |
In vivo animal studies for Gallein are not extensively documented. The compound has been shown to inhibit metastatic spread in models of tumor cells expressing OR51E2. For studying Gβγ signaling and its role in cancer metastasis, typical in vivo models include xenograft or orthotopic tumor models in mice, where Gallein is administered and tumor growth, metastasis, and survival are assessed. However, specific protocols for Gallein in animal models have not been reported.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Gallein are not available in the public domain. The compound has a molecular weight of 364.31 and a formula of C20H12O7. As a xanthene dye, it may have distinct physicochemical properties. Specific ADME parameters including absorption, distribution, metabolism, and excretion have not been characterized. Researchers should perform their own pharmacokinetic studies if in vivo application is intended.
|
| Toxicity/Toxicokinetics |
Toxicity data for Gallein are not extensively reported. As a research compound, comprehensive toxicological evaluations have not been performed. The compound is intended for laboratory research use only and should be handled with standard safety precautions. Appropriate personal protective equipment should be worn when handling this compound. Consult the Material Safety Data Sheet for specific safety and handling information.
|
| References |
[1]. Sanz G, et al. Gallein, a Gβγ subunit signalling inhibitor, inhibits metastatic spread of tumour cells expressing OR51E2 and exposed to its odorant ligand. BMC Res Notes. 2017 Oct 30;10(1):541.
[2]. Lillie RD, et al. Hematoxylin substitutes: gallein as a biological stain. Stain Technol. 1974 Nov;49(6):339-46. |
| Additional Infomation |
Gallein is a xanthan dye belonging to the fluorane class of compounds, with four hydroxyl substituents at positions 3', 4', 5', and 6'. It can be used as a fluorescent dye, histological dye, and G protein-coupled receptor antagonist. Gallein is a γ-lactone, polyphenol, xanthan dye, oxaspirocyclic compound, organic heteropentane compound, and a member of the 2-benzofuran class. Functionally, it is related to fluorane compounds.
Gallein is an inhibitor of G protein βγ subunit-dependent signaling that binds to Gβ1γ2 (IC50 = 200 nM) and inhibits Gβγ-dependent PI3K activation. It has been shown to inhibit metastatic spread of tumor cells expressing OR51E2. Gallein also exhibits anti-inflammatory, antioxidant, and anticancer properties. The compound is a xanthene dye used as a research tool for studying GPCR signaling and Gβγ-mediated pathways. Gallein is not in clinical trials and has not been approved for therapeutic use. |
| Molecular Formula |
C20H12O7
|
|---|---|
| Molecular Weight |
364.31
|
| Exact Mass |
364.058
|
| CAS # |
2103-64-2
|
| PubChem CID |
73685
|
| Appearance |
Light brown to black solid powder
|
| Density |
1.81g/cm3
|
| Boiling Point |
687.4ºC at 760mmHg
|
| Melting Point |
>300°C
|
| Flash Point |
255.2ºC
|
| Vapour Pressure |
1.57E-19mmHg at 25°C
|
| Index of Refraction |
1.865
|
| LogP |
3.077
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
27
|
| Complexity |
579
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC=C2C(=C1)C(=O)OC23C4=C(C(=C(C=C4)O)O)OC5=C3C=CC(=C5O)O
|
| InChi Key |
PHLYOKFVXIVOJC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H12O7/c21-13-7-5-11-17(15(13)23)26-18-12(6-8-14(22)16(18)24)20(11)10-4-2-1-3-9(10)19(25)27-20/h1-8,21-24H
|
| Chemical Name |
3',4',5',6'-tetrahydroxyspiro[2-benzofuran-3,9'-xanthene]-1-one
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 33.33 mg/mL (91.49 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7449 mL | 13.7246 mL | 27.4492 mL | |
| 5 mM | 0.5490 mL | 2.7449 mL | 5.4898 mL | |
| 10 mM | 0.2745 mL | 1.3725 mL | 2.7449 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
