| 货号 | 14761-1mg |
| 描述 | Gambogic acid (GA) is a natural product isolated from the G. hanburyi tree that exhibits anti-cancer activity by acting on a variety of cellular pathways. In the apoptotic pathway, GA activates caspases (EC50 = 0.78 µM), inhibits binding of anti-apoptotic proteins to a BH3 peptide (IC50 = 1.47, 1.21, 2.02, 0.66, 1.06, 0.79 μM for Bcl-xL, Bcl-2, Bcl-W, Bcl-B, Bfl-1, Mcl-1, respectively), and alters expression of Bcl-2 and Bax.1,2,3 GA binds to the transferrin receptor (IC50 = 4.1 µM), inducing apoptosis in various tumor cell lines.4 It is a potent, slow inhibitor of Kir2.1 channels (IC50=<100 nM).5 GA inhibits the chymotrypsin activity of the 20S proteasome in a dose-dependent manner.6 A novel mechanism for GA cytotoxic effects in glioma cells may be through AMPK-initiated effects on EGFR and Akt/mTORC1 signaling.7 |
| 别名 | GA;β-Guttiferin; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Zhang, H.Z.,Kasibhatla, S.,Wang, Y., et al. Discovery, characterization and SAR of gambogic acid as a potent apoptosis inducer by a HTS assay. Bioorganic & Medicinal Chemistry 12(2), 309-317 (2004). 2.Zhai, D.,Jin, C.,Shiau, C.W., et al. Gambogic acid is an antagonist of anti-apoptotic Bcl-2-family proteins. Molecular Cancer Therapeutics 7(6), 1639-1646 (2008). 3.Zhao, L.,Guo, Q.L.,You, Q.D., et al. Gambogic acid induces apoptosis and regulates expressions of Bax and Bcl-2 protein in human gastric carcinoma MGC-803 cells. Biological and Pharmaceutical Bullentin 27(7), 998-1003 (2004). 4.Kasibhatla, S.,Jessen, K.A.,Maliartchouk, S., et al. A role for transferrin receptor in triggering apoptosis when targeted with gambogic acid. Proceedings of the National Academy of Sciences of the United States of America 102(34), 12095-12100 (2005). 5.Zaks-Makhina, E.,Li, H.,Grishin, A., et al. Specific and slow inhibition of the Kir2.1 K+ channel by gambogic acid. The Journal of Biological Chemisty 284(23), 15432-15438 (2009). 6.Felth, J.,Lesiak-Mieczkowska, K.,DArcy, P., et al. Gambogic acid is cytotoxic to cancer cells through inhibition of the ubiquitin-proteasome system. Investigational New Drugs 31(3), 587-598 (2013). 7.He, X.y.,Liu, X.j.,Chen, X., et al. Gambogic acid induces EGFR degradation and Akt/mTORC1 inhibition through AMPK dependent-LRIG1 upregulation in cultured U87 glioma cells. Biochemical and Biophysical Research Communications 435(3), 397-402 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% (mixture of epimers) |
| 计算分子量 | 628.8 |
| 分子式 | C38H44O8 |
| CAS号 | 2752-65-0 |
| 稳定性 | ≥ 2 years |
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