"目录号: HY-15359
Episilvestrol是Silvestrol的衍生物，能在不激活caspase-3或-7的情况下，诱导LNCaP细胞凋亡。同时是 5'myc-UTR-LUC 抑制剂，IC50为0.8 nM。
相关产品
Cisplatin-Adarotene-Epibrassinolide-Elesclomol-Betulinic acid-Myricetin-Apoptosis Activator 2-Betulin-Cholesterol myristate-NSC348884-SMIP004-Taurochenodeoxycholic acid-(E)-[6]-Dehydroparadol-Baohuoside I-Bisdemethoxycurcumin-
生物活性
Description
Episilvestrol is a derivative of Silvestrol, which can induce apoptosis in LNCaP cells through the mitochondrial/apoptosome pathway without activation of executioner caspase-3 or -7; 5'myc-UTR-LUC inhibtior (IC50= 0.8 nM).IC50 value:Target: Apoptosis inducerin vitro: Silvestrol induced an apoptotic response, disrupted the mitochondrial trans-membrane potential and caused cytochrome c release into the cytoplasm. Immunoblot analysis indicated that, at the protein level, silvestrol produced an increase of Bcl-xl phosphorylation with a concomitant increase of bak. Furthermore, caspase-2, -9 and -10 appeared to be involved in silvestrol-mediated apoptosis. In contrast, the involvement of caspase-3 and -7 was not detected, either by immunoblot or caspase-3/-7-like activity analysis, indicating that these pathways do not play a crucial role in silvestrol-induced apoptosis [1]. The ability of silvestrol and analogues to selectively inhibit the translation of proteins with high requirement on the translation-initiation machinery (i.e., complex 5'-untranslated region UTR) relative to simple 5'UTR was determined by a cellular reporter assay. Simplified analogues of silvestrol such as compounds 74 and 76 were shown to have similar cytotoxic potency and better ADME characteristics relative to those of silvestrol [2].in vivo:
References
