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专注多肽 服务科研
编号: | 160564 |
中文名称: | 三肽Z-Val-Ala-DL-Asp-fluoromethylketone |
CAS号: | 220644-02-0 |
单字母: | Z-VAd-FMK |
三字母: | Cbz N端Cbz保护,苄氧羰基(Cbz,Z) -ValL-缬氨酸:valine。系统命名为(2S)-氨基-3-甲基丁酸。是编码氨基酸。是哺乳动物的必需氨基酸。符号:V,Val。在某些放线菌素如缬霉素中存在 D-缬氨酸。 -Ala丙氨酸:alanine。L-丙氨酸的系统命名为(2S)-氨基丙酸,是编码氨基酸,也叫L-α-丙氨酸。符号:A,Ala。D-丙氨酸存在于多种细菌细胞壁的糖肽中。β-丙氨酸是维生素泛酸和辅酶A的组分。 -DAspD型天冬氨酸 -FMKC端氟甲基酮修饰,Fluoromethylketone (FMK) |
氨基酸个数: | 3 |
分子式: | C21H28O7N3F1 |
平均分子量: | 453.46 |
精确分子量: | 453.19 |
等电点(PI): | - |
pH=7.0时的净电荷数: | -1 |
平均亲水性: | 0.33333333333333 |
疏水性值: | 0.83 |
消光系数: | - |
来源: | 人工化学合成,仅限科学研究使用,不得用于人体。 |
储存条件: | 负80℃至负20℃ |
标签: | D型氨基酸肽 CBZ修饰肽 三肽 FMK修饰肽 |
zVAD-FMK inhibited apoptosis induced by diverse stimuli. Preincubation of cells with this caspase-1 (ICE) inhibitor (50 µM) almost completely inhibited the formation of large kilobase-pair fragments of DNA, a characteristic biochemical change associated with apoptosis. Z-VAD-FMK was shown to irreversibly inhibit most types of caspases, hence it is also called pan-caspase inhibitor. For a cell-permeable analog see N-1560. Inhibitor of peptide:N-glycanase (PNGase).
Z-Val-Ala-DL-Asp-fluoromethylketone is a drug that is used for the treatment of cancer. It can be used in combination with other chemotherapeutic drugs, such as z-vad-fmk, to induce apoptosis in cancer cells. Z-Val-Ala-DL-Asp-fluoromethylketone also inhibits autophagy and neuronal death by inhibiting caspase activation, which prevents the release of proapoptotic proteins from mitochondria into the cytosol. This drug has been shown to have antiinflammatory effects on IL2 receptor signaling pathways and inhibits the production of proinflammatory cytokines by binding to IL2.
很多蛋白在细胞中非常容易被降解,或被标记,进而被选择性地破坏。但含有部分D型氨基酸的多肽则显示了很强的抵抗蛋白酶降解能力。
DOI | 名称 | |
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10.1016/j.chembiol.2004.11.010 | Using a small molecule inhibitor of peptide: N-glycanase to probe its role in glycoprotein turnover | 下载 |
10.1038/sj.cdd.4401716 | z-VAD-fmk inhibits peptide:N-glycanase and may result in ER stress | 下载 |
10.2337/db06-1653 | Caspase inhibitor therapy enhances marginal mass islet graft survival and preserves long-term function in islet transplantation | 下载 |
10.1038/ncb955 | Cytoprotective membrane-permeable peptides designed from the Bax-binding domain of Ku70 | 下载 |