Eurycomalactone 是一种NF-Κb抑制剂,IC50=0.5 μM,是一种天然产物。它可抑制蛋白合成,降低 cyclin D1 蛋白水平,但对 TNFα 诱导的 IκBα 降解或 IKKα/β 和 IκBα 的磷酸化水平没有作用。
产品描述
Eurycomalactone is a natural product isolated from Eurycoma longifolia Jack., acts as a potent NF-κB inhibitor( IC50 of 0.5 μM). Eurycomalactone inhibits protein synthesis, depletes cyclin D1, but does not affect TNFα-induced degradation of IκBα or the phosphorylation of IKKα/β and IκBα.
体外活性
Eurycomalactone (ECL), an active quassinoid isolated from Eurycoma longifolia Jack, has been demonstrated to possess anticancer activity.?ECL exhibited selective cytotoxicity against the NSCLC cells A549 and COR-L23 compared to the normal lung fibroblast.?Clonogenic survival results indicated that ECL treatment prior to irradiation synergistically decreased the A549 and COR-L23 colony number.?ECL treatment reduced the expression of cyclin B1 and CDK1/2 leading to induce cell cycle arrest at the radiosensitive G /M phase.?Moreover, ECL markedly delayed the repair of radiation-induced DNA double-strand breaks (DSBs).?In A549 cells, pretreatment with ECL not only delayed the resolving of radiation-induced γ-H2AX foci but also blocked the formation of 53BP1 foci at the DSB sites.?In addition, ECL pretreatment attenuated the expression of DNA repair proteins Ku-80 and KDM4D in both NSCLC cells.?Consequently, these effects led to an increase in apoptosis in irradiated cells.?Thus, ECL radiosensitized the NSCLC cells to X-ray via G /M arrest induction and delayed the repair of X-ray-induced DSBs. It has?a great potential for ECL as an alternative safer radiosensitizer for increasing the RT efficiency against NSCLC[2].
Cas No.
23062-24-0
分子式
C19H24O6
分子量
348.39
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years