Gambogic Acid An apoptosis inducer in sever tumor cell lines via regulation of Bax and inhibition of Bcl-2 genes

Gambogic Acid (CAS 2752-65-0)

Gambogic Acid | CAS 2752-65-0 is rated 5.0 out of 5 by 1.
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Synonym: Cambogic acid
Application: An apoptosis inducer in sever tumor cell lines via regulation of Bax and inhibition of Bcl-2 genes
CAS Number: 2752-65-0
Purity: ≥97%
Molecular Weight: 628.75
Molecular Formula: C38H44O8
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Gambogic Acid, a natural product originally isolated from Garcinia hanburyi, is a cell-permeable caspase activator. It has been shown to induce apoptosis in proliferative cells independent of cell cycle. Mechanistic studies suggest that Gambogic acid causes a decrease of Bcl-2 gene and an increase in Bax gene expression, which may result in apoptosis. Additionally, this compound has been noted to bind CD71 (transferrin receptors) and prevent their internalization, which causes induction of cell death. Gambogic Acid is an inhibitor of A1 and Bcl-2 family proteins, including Bcl-xl, Bcl-2, Bcl-w, Bcl-B, Bfl-1, and Mcl-1. Has shown to cause apoptosis in T47D breast cancer cells and MGC-803 human gastric carcinoma cells.


References

1. Zhao, L., et al. 2004. Biol. Pharm. Bull. 27: 998-1003. PMID: 15256729
2. Zhang, H.Z., et al. 2004. Bioorg. Med. Chem. 12: 309-317. PMID: 14723951
3. Kasibhatla, S., et al. 2005. Proc. Natl. Acad. Sci. U.S.A. 102: 12095-12100. PMID: 16103367

Appearance :
Crystalline powder
Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml), and ethanol (25 mg/ml). Insoluble in water.
Storage :
Store at -20° C
Boiling Point :
808.94° C at 760 mmHg
Density :
1.30 g/cm3
Refractive Index :
n20D 1.63
IC50 :
Bcl-XL: IC50 = 1.47 µM; Bcl-2: IC50 = 1.21 µM; Bcl-W: IC50 = 2.02 µM; Bcl-B: IC50 = 0.66 µM; Bfl-1: IC50 = 1.06 µM; Mcl-1: IC50 = 0.79 µM; Activates caspases: EC5050 = 0.78 - 1.64 µM; KIR2.1 channels: EC5050 = ≤ 100 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
1
RTECS :
PB9268200
PubChem CID :
5281632
Merck Index :
14: 4361
SMILES :
CC(=CCC[C@@]1(C=CC2=C(O1)C(=C3C(=C2O)C(=O)C4=CC5CC6[C@@]4(O3)C(C5=O)(OC6(C)C)C/C=C(/C)\\C(=O)O)CC=C(C)C)C)C

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Certificate of Analysis

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Gambogic Acid  Product Citations

See how others have used Gambogic Acid. Click on the entry to view the PubMed entry .

Citations 1 to 5 of 5 total

PMID: # 26701717  Doddapaneni, R. et al. 2016. Drug Deliv. 23: 1232-41.

PMID: # 26622796  Wang, C. et al. 2015. Oncology letters. 10: 2063-2066.

PMID: # 24623960  Cascão, R. et al. 2014. Mediators of inflammation. 2014: 195327.

PMID: # 23918355  Lee, MO. et al. 2013. Proc. Natl. Acad. Sci. U.S.A. 110: E3281-90.

PMID: # 23047550  2012. Br. J. Cancer. 107: 1702-13.

Citations 1 to 5 of 5 total
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Rated 5 out of 5 by from Wen Wen, et al. (PubMed ID 26397804) found that gambogic acid inhibits the growth and induces apoptosis in human colorectal cancer cells. It also has been reported to over come drug resistance. -SCBT Publication Review
Date published: 2015-01-18
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