| 货号 | 3590/50 |
| 别名 | (2Z)-2-Methyl-4-[(1R,3aS,5S,11R,14a |
| 供应商 | Tocris |
| 生物活性 | 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). |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 计算分子量 | 628.75 |
| 分子式 | C38H44O8 |
| 可溶性/溶解性 | Soluble to 75 mM in DMSO and to 100 mM in ethanol |
| CAS号 | 2752-65-0 |
| 参考文献 | Wanget 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. Zaks-Makhinaet al (2009) Specific and slow inhibition of the Kir2.1 K+ channel by Gambogic acid. J.Biol.Chem. 284 15432. PMID: 19366693. Qiet al (2008) Anti-invasive effect of gambogic acid in MDA-MB-231 human breast carcinoma cells. Biochem.Cell Biol. 86 386. PMID: 18923540. Zhaiet al (2008) Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. Mol.Cancer Ther. 7 1639. PMID: 18566235. Zhanget 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. |