Gambogenic acid 是黄藤中的有效成分,具有抗癌活性。Gambogenic acid 为有效的 EZH2 抑制剂,特异性地与 EZH2-SET 结构域的 Cys668 位点共价结合,诱导 EZH2 泛素化。
Cas No. | 173932-75-7 |
别名 | 新藤黄酸 |
Canonical SMILES | O=C(O)/C(C)=C\C[C@@]1(C2=O)OC(C)(C)[C@]([C@]31OC4=C5C(O)=C(C/C=C(C)/CC/C=C(C)\C)C(O)=C4C/C=C(C)\C)([H])C[C@@]2([H])C=C3C5=O |
分子式 | C38H46O8 |
分子量 | 630.77 |
溶解度 | DMSO: 250 mg/mL (396.34 mM) |
储存条件 | 4°C, protect from light |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination[1]. [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. |