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Submit ReviewGambogic acid
Description: Apoptosis inducer. Activates caspases and inhibits Bcl-2 family proteins
Chemical Name: (2Z)-2-Methyl-4-[(1R,3aS,5S,11R,14aS)-3a,4,5,7-tetrahydro-8-hydroxy-3,3,11-trimethyl-13-(3-methyl-2-butenyl)-11-(4-methyl-3-pentenyl)-7,15-dioxo-1,5-methano-1H,3H,11H-furo[3,4-g]pyrano[3,2-b]xanthen-1-yl]-2-butenoic acid
Biological Activity for Gambogic acid
Gambogic acid is an apoptosis inducer in several tumor cell lines including T47D cells. Activates caspases (EC50 values are 0.78 - 1.64 μM) and competitively inhibits antiapoptotic Bcl-2 family proteins (IC50 values are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 respectively). Reverses gefitinib-resistance in mice bearing tumors with EGFR-T790M mutation. Also blocks Kir2.1 channels (EC50 ≤ 100 nM).
Technical Data for Gambogic acid
| M. Wt | 628.75 |
| Formula | C38H44O8 |
| Storage | Store at -20°C |
| CAS Number | 2752-65-0 |
| PubChem ID | 15559465 |
| InChI Key | GEZHEQNLKAOMCA-MYCCNKBCSA-N |
| Smiles | C/C(C)=C/CC[C@@](C=C2)(C)OC1=C2C(O)=C(C(C([C@]45O3)=C[C@H](C[C@@H]56)C([C@](OC(C)6C)4C/C=C(C(O)=O)/C)=O)=O)C3=C1C/C=C(C)/C |
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.
Product Datasheets for Gambogic acid
References for Gambogic acid
References are publications that support the biological activity of the product.
Zhang et al (2004) Discovery, characterization and SAR of gambogic acid as a potent apoptosis inducer by a HTS assay. Bioorg.Med.Chem. 12 309 PMID: 14723951
Zhai et al (2008) Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. Mol.Cancer Ther. 7 1639 PMID: 18566235
Qi et al (2008) Anti-invasive effect of gambogic acid in MDA-MB-231 human breast carcinoma cells. Biochem.Cell Biol. 86 386 PMID: 18923540
Zaks-Makhina et al (2009) Specific and slow inhibition of the Kir2.1 K+ channel by Gambogic acid. J.Biol.Chem. 284 15432 PMID: 19366693
Wang et al (2015) Combined therapy with EGFR TKI and gambogic acid for overcoming resistance in EGFR-T790M mutant lung cancer. Oncol.Lett. 10 2063 PMID: 26622796
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Keywords: Gambogic acid, Gambogic acid supplier, Apoptosis, inducers, activates, activators, caspases, inhibits, Bcl-2, family, proteins, inhibitors, KIR2.1, channels, blockers, inward, rectifier, Potassium, K+, proteases, proteinases, Inducers, Family, Caspases, Inward, Channels, 3590, Tocris Bioscience
3 Citations for Gambogic acid
Citations are publications that use Tocris products. Selected citations for Gambogic acid include:
Tan et al (2015) Brown Adipose Tissue Thermogenic Capacity Is Regulated by Elovl6. Proc Natl Acad Sci U S A 13 2039 PMID: 26628376
Mathieu et al (2014) Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737. J Biomol Screen 19 1035 PMID: 24809353
Kühn et al (2013) Label-free cytotoxicity screening assay by digital holographic microscopy. Assay Drug Dev Technol 11 101 PMID: 23062077
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Literature in this Area
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Programmed Cell Death Poster
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
Pathways for Gambogic acid
