Gambogic acid

• Supplier: Tocris Bioscience
• Catalog: 2085
• Prices: $115.00, $485.00
• Sizes: 10 mg, 50 mg
• Function Type: Inducer
• Cas Number: 2752-65-0
• 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-butenoicacid
• Formula: C38H44O8
• Molecular Weight: 628.75
• Description: Apoptosis inducer in several tumor cell lines including T47D cells. Activates caspases (EC 50 values are 0.78 - 1.64 μ M) and competitively inhibits antiapoptotic Bcl-2 family proteins (IC 50 values are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μ M 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 K ir 2.1 channels (EC 50 ≤ 100 nM).

Product References

Discovery, characterization and SAR of gambogic acid as a potent apoptosis - Discovery, characterization and SAR of gambogic acid as a potent apoptosis

Zhang HZ, Kasibhatla S, Wang Y, Herich J, Guastella J, Tseng B, Drewe J, Cai SX. Bioorg Med Chem. 2004 Jan 15;12(2):309-17.

Anti-invasive effect of gambogic acid in MDA-MB-231 human breast carcinoma cells. - Anti-invasive effect of gambogic acid in MDA-MB-231 human breast carcinoma cells.

Qi Q, Lu N, Wang XT, Gu HY, Yang Y, Liu W, Li C, You QD, Guo QL. Biochem Cell Biol. 2008 Oct;86(5):386-95.

Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. - Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins.

Zhai D, Jin C, Shiau CW, Kitada S, Satterthwait AC, Reed JC. Mol Cancer Ther. 2008 Jun;7(6):1639-46.

Specific and slow inhibition of the kir2.1 K+ channel by gambogic acid. - Specific and slow inhibition of the kir2.1 K+ channel by gambogic acid.

Zaks-Makhina E, Li H, Grishin A, Salvador-Recatala V, Levitan ES. J Biol Chem. 2009 Jun 5;284(23):15432-8.