For research use only. Not for therapeutic Use.
Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer[1][2].
Gambogenic acid (0.6-2.4 µM, 1.2-3.2 µM; 24-72 h) inhibits the proliferation of SCLC cell lines (NCI-H446/NCI-H1688)[2].
Gambogenic acid (0.6-1.2 µM, 1.5-2.2 µM; 24 h) arrests cell cycle at various stages in SCLC cell lines (NCI-H446/NCI-H1688)[2].
Gambogenic acid (1.4-2 µM, 2.4-3 µM; 24 h) increases the rate of cell apoptosis in a dose-dependent manner in SCLC cell lines (NCI-H446/NCI-H1688)[2].
Gambogenic acid (4-12 mg/kg, i.v., every 2 days, 14 days) inhibits tumor growth in SCLC mouse xenograft model[2].
| Catalog Number | I017925 |
| CAS Number | 173932-75-7 |
| Synonyms | (Z)-4-[(1S,2S,13S,15R)-7-[(2E)-3,7-dimethylocta-2,6-dienyl]-6,8-dihydroxy-17,17-dimethyl-5-(3-methylbut-2-enyl)-10,14-dioxo-3,16-dioxapentacyclo[11.4.1.02,11.02,15.04,9]octadeca-4,6,8,11-tetraen-15-yl]-2-methylbut-2-enoic acid |
| Molecular Formula | C38H46O8 |
| Purity | ≥95% |
| InChI | InChI=1S/C38H46O8/c1-20(2)10-9-11-22(5)13-15-25-30(39)26(14-12-21(3)4)33-29(31(25)40)32(41)27-18-24-19-28-36(7,8)46-37(34(24)42,38(27,28)45-33)17-16-23(6)35(43)44/h10,12-13,16,18,24,28,39-40H,9,11,14-15,17,19H2,1-8H3,(H,43,44)/b22-13+,23-16-/t24-,28+,37+,38-/m1/s1 |
| InChIKey | RCWNBHCZYXWDOV-VSFMGBBVSA-N |
| SMILES | CC(=CCCC(=CCC1=C(C(=C2C(=C1O)C(=O)C3=CC4CC5C3(O2)C(C4=O)(OC5(C)C)CC=C(C)C(=O)O)CC=C(C)C)O)C)C |
| Reference | [1]. Wang X, et al. A covalently bound inhibitor triggers EZH2 degradation through CHIP-mediated ubiquitination. EMBO J. 2017 May 2;36(9):1243-1260. [2]. Huang T, et al. Gambogenic acid inhibits the proliferation of small‑cell lung cancer cells by arresting the cell cycle and inducing apoptosis. Oncol Rep. 2019 Mar;41(3):1700-1706. |
