Gambogic Acid
Based on 6 publication(s) in Google Scholar
Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.
For research use only. We do not sell to patients.
- Purity: 98.34%
- CAS No.: 2752-65-0
- Formula: C38H44O8
- Molecular Weight:628.75
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Gambogic Acid
More-
Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Flow Cytometry
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Cell Proliferation/Viability Assay
Biological Activity
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Bcl-B 0.66 μM (IC50) |
Mcl-1 0.79 μM (IC50) |
Bfl-1 1.06 μM (IC50) |
Bcl-2 1.21 μM (IC50) |
Bcl-xL 1.47 μM (IC50) |
Bcl-W 2.02 μM (IC50) |
Autophagy |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
5.81 μM
Compound: gambogic acid, GA
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Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
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[PMID: 18996626] |
| A549 | IC50 |
3.65 μM
Compound: GA
|
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
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[PMID: 20605273] |
| A549 | IC50 |
1.1 μM
Compound: GA
|
Antiproliferative activity against human A549 cells after 24 hrs by MTT assay
Antiproliferative activity against human A549 cells after 24 hrs by MTT assay
|
[PMID: 22472167] |
| A549 | IC50 |
0.5 μg/mL
Compound: GA
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Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
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[PMID: 22595179] |
| A549 | IC50 |
1.1 μM
Compound: 1, GA
|
Cytotoxicity against human A549 cells assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as cell viability after 24 hrs by MTT assay
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[PMID: 23167526] |
| A549 | IC50 |
1.1 μM
Compound: GA
|
Cytotoxicity against human A549 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as growth inhibition after 24 hrs by MTT assay
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[PMID: 25958244] |
| A549 | IC50 |
3.4 μM
Compound: 4
|
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 to 48 hrs by Presto Blue assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 to 48 hrs by Presto Blue assay
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[PMID: 27216998] |
| A549 | IC50 |
1.2 μM
Compound: 1; GA
|
Antiproliferative activity against human A549 cells assessed as growth inhibition by MTT assay
Antiproliferative activity against human A549 cells assessed as growth inhibition by MTT assay
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[PMID: 27527413] |
| A549 | IC50 |
1.47 μM
Compound: GA
|
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
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[PMID: 31047774] |
| A549 | IC50 |
0.29 μM
Compound: Gambogic acid
|
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 31546197] |
| A549/CDDP | IC50 |
0.29 μM
Compound: Gambogic acid
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Antiproliferative activity against human A549/CDDP cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human A549/CDDP cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 31546197] |
| A549/TR | IC50 |
0.29 μM
Compound: Gambogic acid
|
Antiproliferative activity against human A549/TR cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human A549/TR cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 31546197] |
| Bel-7402 | IC50 |
3.31 μM
Compound: gambogic acid, GA
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Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay
Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay
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[PMID: 18996626] |
| Bel-7402 | IC50 |
2.08 μM
Compound: GA
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Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay
Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay
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[PMID: 20605273] |
| Bel-7402 | IC50 |
0.75 μM
Compound: 1, GA
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Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay
Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay
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[PMID: 22153338] |
| BEL-7404 tumor cell line | IC50 |
4.7 μM
Compound: 1, GA
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Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay
Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay
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[PMID: 22153338] |
| BGC-823 | IC50 |
4.51 μM
Compound: gambogic acid, GA
|
Cytotoxicity against human BGC823 cells after 48 hrs by MTT assay
Cytotoxicity against human BGC823 cells after 48 hrs by MTT assay
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[PMID: 18996626] |
| BGC-823 | IC50 |
2.83 μM
Compound: GA
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Cytotoxicity against human BGC823 cells after 48 hrs by MTT assay
Cytotoxicity against human BGC823 cells after 48 hrs by MTT assay
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[PMID: 20605273] |
| BGC-823 | IC50 |
2.35 μM
Compound: 1, GA
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Antiproliferative activity against human BGC823 cells after 24 hrs by MTT assay
Antiproliferative activity against human BGC823 cells after 24 hrs by MTT assay
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[PMID: 21334116] |
| BJ | EC50 |
0.21 μM
Compound: Gambogic acid
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Cytotoxicity against human BJ cells
Cytotoxicity against human BJ cells
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[PMID: 25316317] |
| Breast carcinoma cell | IC50 |
0.42 μM
Compound: GBA; 1
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Cytotoxicity against patient derived inflammatory breast cancer cell spheroids assessed as increase in spheroid dissolution incubated for 24 hrs by propidium iodide/Acridine orange staining based dual-fluorescence viability assay
Cytotoxicity against patient derived inflammatory breast cancer cell spheroids assessed as increase in spheroid dissolution incubated for 24 hrs by propidium iodide/Acridine orange staining based dual-fluorescence viability assay
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[PMID: 30831408] |
| DU-145 | IC50 |
0.3 μg/mL
Compound: GA
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Cytotoxicity against human DU145 cells by MTT assay
Cytotoxicity against human DU145 cells by MTT assay
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[PMID: 22595179] |
| HCT-116 | EC50 |
0.7 μM
Compound: 1, GA
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Induction of apoptosis in human HCT116 cells assessed as caspase 3 activation after 24 hrs
Induction of apoptosis in human HCT116 cells assessed as caspase 3 activation after 24 hrs
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[PMID: 18337106] |
| HCT-116 | GI50 |
0.1 μM
Compound: 1, GA
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Growth inhibition of human HCT116 cells after 48 hrs by CellTiter-Glo assay
Growth inhibition of human HCT116 cells after 48 hrs by CellTiter-Glo assay
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[PMID: 18337106] |
| HCT-116 | IC50 |
3.11 μM
Compound: GA
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Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay
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[PMID: 31047774] |
| HCT-116 | IC50 |
0.29 μM
Compound: Gambogic acid
|
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 31546197] |
| HEK293 | EC50 |
0.21 μM
Compound: Gambogic acid
|
Cytotoxicity against HEK293 cells
Cytotoxicity against HEK293 cells
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[PMID: 25316317] |
| HEK293 | IC50 |
1.72 μM
Compound: 4
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Cytotoxicity against human HEK293 cells assessed as reduction in cell viability after 24 to 48 hrs by trypan blue dye based fluorescence assay
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability after 24 to 48 hrs by trypan blue dye based fluorescence assay
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[PMID: 27216998] |
| HeLa | IC50 |
0.7 μM
Compound: 6a, R-gambogic acid
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Cytotoxicity against human HeLa cells after 1 to 11 days by MTT assay
Cytotoxicity against human HeLa cells after 1 to 11 days by MTT assay
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[PMID: 19072548] |
| HeLa | GI50 |
1.5 μM
Compound: 1
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Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay
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[PMID: 21486005] |
| HepG2 | IC50 |
2.4 μM
Compound: GA
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Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
|
[PMID: 20338759] |
| HepG2 | IC50 |
2.4 μM
Compound: 1, GA
|
Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay
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[PMID: 21334116] |
| HepG2 | IC50 |
1.17 μM
Compound: 1, GA
|
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
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[PMID: 22153338] |
| HepG2 | IC50 |
0.89 μM
Compound: 1, GA
|
Cytotoxicity against human HepG2 cells assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as cell viability after 24 hrs by MTT assay
|
[PMID: 23167526] |
| HepG2 | EC50 |
<2 μM
Compound: Gambogic acid
|
Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
|
[PMID: 25316317] |
| HepG2 | IC50 |
0.89 μM
Compound: GA
|
Cytotoxicity against human HepG2 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 25958244] |
| HepG2 | IC50 |
2.19 μM
Compound: 1; GA
|
Antiproliferative activity against human HepG2 cells assessed as growth inhibition by MTT assay
Antiproliferative activity against human HepG2 cells assessed as growth inhibition by MTT assay
|
[PMID: 27527413] |
| HepG2 | IC50 |
1.55 μM
Compound: Gambogic acid
|
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
|
[PMID: 30594028] |
| HepG2 | IC50 |
2.36 μM
Compound: GA
|
Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay
|
[PMID: 31047774] |
| HepG2 | IC50 |
0.29 μM
Compound: Gambogic acid
|
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 31546197] |
| HL-60 | GI50 |
0.3 μM
Compound: Gambogic acid
|
Growth inhibition of human HL60 cells measured after 3 days by trypan blue assay
Growth inhibition of human HL60 cells measured after 3 days by trypan blue assay
|
[PMID: 29565129] |
| HL-60 | IC50 |
0.17 μM
Compound: 54
|
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 3 days by trypan blue dye based hemocytometer counting method
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 3 days by trypan blue dye based hemocytometer counting method
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[PMID: 30830783] |
| HT-29 | IC50 |
5.61 μM
Compound: gambogic acid, GA
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Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
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[PMID: 18996626] |
| HT-29 | IC50 |
3.52 μM
Compound: GA
|
Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
|
[PMID: 20605273] |
| HT-29 | ED50 |
0.48 μM
Compound: 1
|
Anticancer activity aganist human HT-29 cells
Anticancer activity aganist human HT-29 cells
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[PMID: 21067206] |
| HT-29 | IC50 |
2.37 μM
Compound: 1; GA
|
Antiproliferative activity against human HT-29 cells assessed as growth inhibition by MTT assay
Antiproliferative activity against human HT-29 cells assessed as growth inhibition by MTT assay
|
[PMID: 27527413] |
| K562 | GI50 |
0.6 μM
Compound: Gambogic acid
|
Growth inhibition of human K562 cells measured after 3 days by trypan blue assay
Growth inhibition of human K562 cells measured after 3 days by trypan blue assay
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[PMID: 29565129] |
| K562 | IC50 |
0.62 μM
Compound: Gambogic acid
|
Antiproliferative activity against imatinib resistant human K562 cells assessed as cell growth inhibition measured after 48 to 72 hrs by MTS assay
Antiproliferative activity against imatinib resistant human K562 cells assessed as cell growth inhibition measured after 48 to 72 hrs by MTS assay
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[PMID: 35551036] |
| KB | IC50 |
0.3 μg/mL
Compound: GA
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Cytotoxicity against human KB cells by MTT assay
Cytotoxicity against human KB cells by MTT assay
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[PMID: 22595179] |
| MCF7 | IC50 |
0.5 μM
Compound: GA
|
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
|
[PMID: 20338759] |
| MCF7 | IC50 |
2.19 μM
Compound: 1, GA
|
Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
|
[PMID: 21334116] |
| MCF7 | GI50 |
2 μM
Compound: 1
|
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay
|
[PMID: 21486005] |
| MCF7 | IC50 |
1.25 μM
Compound: 1; GA
|
Antiproliferative activity against human MCF7 cells assessed as growth inhibition by MTT assay
Antiproliferative activity against human MCF7 cells assessed as growth inhibition by MTT assay
|
[PMID: 27527413] |
| MDA-MB-231 | IC50 |
1.33 μM
Compound: GA
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Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
|
[PMID: 31047774] |
| MKN-45 | IC50 |
4.27 μM
Compound: GA
|
Antiproliferative activity against human MKN45 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MKN45 cells incubated for 72 hrs by MTT assay
|
[PMID: 31047774] |
| PC-3 | IC50 |
1.19 μM
Compound: 1; GA
|
Antiproliferative activity against human PC3 cells assessed as growth inhibition by MTT assay
Antiproliferative activity against human PC3 cells assessed as growth inhibition by MTT assay
|
[PMID: 27527413] |
| Raji | EC50 |
0.24 μM
Compound: Gambogic acid
|
Cytotoxicity against human Raji cells
Cytotoxicity against human Raji cells
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[PMID: 25316317] |
| SGC-7901 | IC50 |
1.47 μM
Compound: GA
|
Cytotoxicity against human SGC7901 cells after 48 hrs by MTT assay
Cytotoxicity against human SGC7901 cells after 48 hrs by MTT assay
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[PMID: 20338759] |
| SK-BR-3 | GI50 |
0.8 μM
Compound: 1
|
Antiproliferative activity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay
Antiproliferative activity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by cell titer 96 assay
|
[PMID: 21486005] |
| SK-BR-3 | IC50 |
0.89 μM
Compound: 1; GA
|
Antiproliferative activity against human SK-BR-3 cells assessed as growth inhibition by MTT assay
Antiproliferative activity against human SK-BR-3 cells assessed as growth inhibition by MTT assay
|
[PMID: 27527413] |
| SK-OV-3 | IC50 |
3.06 μM
Compound: gambogic acid, GA
|
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
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[PMID: 18996626] |
| SMMC-7721 | IC50 |
3.2 μM
Compound: 1, GA
|
Antiproliferative activity against human SMMC7721 cells after 24 hrs by MTT assay
Antiproliferative activity against human SMMC7721 cells after 24 hrs by MTT assay
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[PMID: 21334116] |
| SMMC-7721 | IC50 |
1.13 μM
Compound: 1, GA
|
Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay
Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay
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[PMID: 22153338] |
| SNU-398 | EC50 |
0.7 μM
Compound: 1, GA
|
Induction of apoptosis in human SNU398 cells assessed as caspase 3 activation after 24 hrs
Induction of apoptosis in human SNU398 cells assessed as caspase 3 activation after 24 hrs
|
[PMID: 18337106] |
| SNU-398 | GI50 |
0.2 μM
Compound: 1, GA
|
Growth inhibition of human SNU398 cells after 48 hrs by CellTiter-Glo assay
Growth inhibition of human SNU398 cells after 48 hrs by CellTiter-Glo assay
|
[PMID: 18337106] |
| T47D | EC50 |
0.7 μM
Compound: 1, GA
|
Induction of apoptosis in human T47D cells assessed as caspase 3 activation after 24 hrs
Induction of apoptosis in human T47D cells assessed as caspase 3 activation after 24 hrs
|
[PMID: 18337106] |
| T47D | GI50 |
0.2 μM
Compound: 1, GA
|
Growth inhibition of human T47D cells after 48 hrs by CellTiter-Glo assay
Growth inhibition of human T47D cells after 48 hrs by CellTiter-Glo assay
|
[PMID: 18337106] |
| T98G | IC50 |
≤300 nM
Compound: GA
|
Antiproliferative activity against human T98G cells after 24 hrs by EZ-Tox assay
Antiproliferative activity against human T98G cells after 24 hrs by EZ-Tox assay
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[PMID: 26631318] |
| U-251 | IC50 |
2.56 μM
Compound: GA
|
Antiproliferative activity against human U251 cells after 24 hrs by MTT assay
Antiproliferative activity against human U251 cells after 24 hrs by MTT assay
|
[PMID: 22472167] |
| U-251 | IC50 |
2.56 μM
Compound: 1, GA
|
Cytotoxicity against human U251 cells assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against human U251 cells assessed as cell viability after 24 hrs by MTT assay
|
[PMID: 23167526] |
| U-251 | IC50 |
2.56 μM
Compound: GA
|
Cytotoxicity against human U251 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human U251 cells assessed as growth inhibition after 24 hrs by MTT assay
|
[PMID: 25958244] |
| U-251 | IC50 |
0.29 μM
Compound: Gambogic acid
|
Antiproliferative activity against human U251 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human U251 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 31546197] |
Gambogic Acid (Beta-Guttiferrin) is a medicinal compound derived from the gamboges resin of the tree, Garcinia hanburyi. Gambogic Acid has documented cytotoxic activity against tumor cell lines in culture, with concentrations required for killing 50% of cells (LD50 of ~1 μM). The activity of Gambogic Acid against the 6 human anti-apoptotic Bcl-2-family proteins is contrasted, using FPAs. Gambogic Acid displaces to various extents FITC-BH3 peptide binding to all 6 proteins, with apparent IC50 1.47 μM for Bcl-XL, 1.21 μM for Bcl-2, 2.02 μM for Bcl-W, 0.66 μM for Bcl-B, 1.06 μM for Bfl-1, and 0.79 μM for Mcl-1[1]. The growth inhibitory effects of Gambogic Acid or Cisplatin (CDDP) on A549, NCI-H460, and NCI-H1299 cells are assessed by the MTT assay after 48?h exposure. A concentration-dependent inhibition of cell growth is observed with Gambogic Acid and CDDP, with IC50s of 3.56±0.36 and 21.88±3.21?μM for A549 cells, 4.05±0.51 and 25.76±4.03?μM for NCI-H460 cells, and 1.12±0.31?μM and 25.21±4.38?μM for NCI-H1299 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2752-65-0
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Appearance Solid
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Molecular Weight 628.75
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Formula C38H44O8
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Color Yellow to orange
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SMILES
O=C(O)/C(C)=C\C[C@@]1(C2=O)OC(C)(C)[C@@](C[C@@]2([H])C=C34)([H])[C@]31OC5=C(C(O)=C(C=C[C@](CC/C=C(C)/C)(C)O6)C6=C5C/C=C(C)\C)C4=O
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Synonyms
Beta-Guttiferrin
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Redox Biol
TrxR1 is involved in the activation of Caspase-11 by regulating the oxidative-reductive status of Trx-1. [Abstract]2024 Sep:75:103277. PMID: 39059206
Gambogic Acid purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Sep:75:103277. [Abstract]
Analysis of LDH release in E. coli-infected J774A.1 cells treated with GA (Gambogic Acid, 0.5-1 μM). n = 3 per group.
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Drug Dev Res
Mechanism of gambogic acid repressing invasion and metastasis of colorectal cancer by regulating macrophage polarization via tumor cell-derived extracellular vesicle-shuttled miR-21. [Abstract]2024 Feb;85(1):e22141. PMID: 38349264
Gambogic Acid purchased from MedChemExpress. Usage Cited in: Drug Dev Res. 2024 Feb;85(1):e22141. [Abstract]
Liver morphology and nodule status in nude mice 4 weeks after intraperitoneal injection of HT-29 cells and GA (Gambogic Acid; 20 mg/kg) treatment. It was observed that compared to the PC + DMSO group, the PC + GA group had fewer liver metastatic nodules.
Gambogic Acid purchased from MedChemExpress. Usage Cited in: Drug Dev Res. 2024 Feb;85(1):e22141. [Abstract]
The percentages of CD68 + CD86 cells and CD68 + CD206 cells were measured by flow cytometry, N = 6. The results displayed that relative to the PC + DMSO group, the levels of CD68+CD86 cells in the PC + GA (Gambogic Acid; 20 mg/kg; i.p.; 4 weeks) group obviously rised, while the levels of CD68+CD206 cells were prominently reduced (all p < .001).
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Sci Rep
BCL2A1 regulates Canady Helios Cold Plasma-induced cell death in triple-negative breast cancer. [Abstract]2022 Mar 8;12(1):4038. PMID: 35260587
Gambogic Acid purchased from MedChemExpress. Usage Cited in: Sci Rep. 2022 Mar 8;12(1):4038. [Abstract]
Viability of TNBC cell line MDA-MB-231 with Gambogic acid, an antagonist of antiapoptotic Bcl-2 family. Bar graph represents MDA-MB-231 MTT cell viability assay after treatment with Gambogic acid (0.06-1 μM) in the combination of with/without CAP treatment at 80p 5 min at 3 L/min He.
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Cell Signal
Gambogic acid induces ferroptosis and suppresses colorectal cancer progression by modulating the m6A modification of p62. [Abstract]2025 Nov:135:112024. PMID: 40721064
Gambogic Acid purchased from MedChemExpress. Usage Cited in: Cell Signal. 2025 Nov:135:112024. [Abstract]
Intracellular Fe2+ levels were measured using the iron ion assay kit in HCT116 after treatment with GA (Gambogic Acid; 0.5-1 μM; 24 h) at different concentrations (HCT116: 0 μM, 0.5 μM, 1 μM; HT29: 0 μM, 0.75 μM, 1.5 μM).
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Cell Adh Migr
Fe3O4 nanoparticles containing gambogic acid inhibit metastasis in colorectal cancer via the RORB/EMILIN1 axis. [Abstract]2024 Dec;18(1):38-53. PMID: 39533963
Solvent & Solubility
DMSO : 50 mg/mL (79.52 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
The in vitro cell viability effects of Gambogic Acid, CDDP alone, or combined treatments are determined by MTT assay. The cells (2×104 cells per mL) are seeded into 96-well culture plates. After overnight incubation, A549 cells are treated with Gambogic Acid (0.44, 0.88, 1.75, 3.5, 7, 10.5 and 14 μM); NCI-H460 cells are treated with Gambogic Acid (0.5, 1, 2, 4, 8, 12 and 16 μM); NCI-H1299 cells are treated with Gambogic Acid (0.125, 0.25, 0.5, 1, 2 and 4 μM). For the combined treatment in NSCLC cells, three sequences are tested: (a) Gambogic Acid followed by CDDP cells are exposed to Gambogic Acid for 48 h, and then after washout of Gambogic Acid, cells are treated with CDDP for an additional 48 h; (b) CDDP followed by Gambogic Acid cells are exposed to CDDP for 48 h, and then after washout of CDDP, cells are treated with Gambogic Acid for an additional 48 h; and (c) concurrent treatment cells are exposed to both Gambogic Acid and ADM for 48 h. The nature of the drug interaction is analysed by using the combination index (CI)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
To determine the in vivo antitumour activity of Gambogic Acid combined with CDDP, viable A549 cells (5×106/100 μL PBS per mouse) are subcutaneously injected into the right flank of 7- to 8-week-old male SCID mice. When the average tumor volume reach 100 mm3, the mice are randomly divided into four treatment groups, including control (saline only, n=5), Gambogic Acid (3.0 mg/kg per 2 days, intravenously; n=6), CDDP (4 mg/kg per week, intravenously; n=6), and sequential combination (CDDP treatment one day before Gambogic Acid treatment, n=6). CDDP (4 mg/kg, weekly) is generally administered at doses less than the maximum-tolerated dose in an attempt to allow any additive effects of combination treatment with platinum-based agents and Gambogic Acid to be more easily detected. Tumor size is measured once every 2 days with a calipre. Body weight is recorded once every 2 days. After 14 days, the mice are killed and the tumors are excised and stored at -80 °C until further analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Zhai D, et al. Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. Mol Cancer Ther. 2008 Jun;7(6):1639-46. [Content Brief]
[2]. Wang LH, et al. Gambogic acid synergistically potentiates cisplatin-induced apoptosis in non-small-cell lung cancer through suppressing NF-κB and MAPK/HO-1 signalling. Br J Cancer. 2014 Jan 21;110(2):341-52. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5905 mL | 7.9523 mL | 15.9046 mL | 39.7614 mL |
| 5 mM | 0.3181 mL | 1.5905 mL | 3.1809 mL | 7.9523 mL | |
| 10 mM | 0.1590 mL | 0.7952 mL | 1.5905 mL | 3.9761 mL | |
| 15 mM | 0.1060 mL | 0.5302 mL | 1.0603 mL | 2.6508 mL | |
| 20 mM | 0.0795 mL | 0.3976 mL | 0.7952 mL | 1.9881 mL | |
| 25 mM | 0.0636 mL | 0.3181 mL | 0.6362 mL | 1.5905 mL | |
| 30 mM | 0.0530 mL | 0.2651 mL | 0.5302 mL | 1.3254 mL | |
| 40 mM | 0.0398 mL | 0.1988 mL | 0.3976 mL | 0.9940 mL | |
| 50 mM | 0.0318 mL | 0.1590 mL | 0.3181 mL | 0.7952 mL | |
| 60 mM | 0.0265 mL | 0.1325 mL | 0.2651 mL | 0.6627 mL |