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一种细胞渗透性不可逆的前蛋白转化酶位点1蛋白酶抑制剂（S1P，也称为枯草杆菌蛋白酶kexin同工酶，SKI-1）。
编号：152418
CAS号：911379-57-2
单字母：Decy-RRLL-CMK
| 编号: | 152418 |
| 中文名称: | Decanoyl-Arg-Arg-Leu-Leu-chloromethylketone |
| CAS号: | 911379-57-2 |
| 单字母: | Decy-RRLL-CMK |
| 三字母: | Decy 癸酸修饰、癸酰化 -ArgL-精氨酸：arginine。系统命名为(2S)-氨基-5-胍基戊酸。在生理条件下带正电荷，为编码氨基酸。是幼小哺乳动物的必需氨基酸。符号：R，Arg。 -ArgL-精氨酸：arginine。系统命名为(2S)-氨基-5-胍基戊酸。在生理条件下带正电荷，为编码氨基酸。是幼小哺乳动物的必需氨基酸。符号：R，Arg。 -LeuL-亮氨酸：leucine。系统命名为(2S)-氨基-4-甲基戊酸。是编码氨基酸。是哺乳动物的必需氨基酸。符号：L，Leu。 -LeuL-亮氨酸：leucine。系统命名为(2S)-氨基-4-甲基戊酸。是编码氨基酸。是哺乳动物的必需氨基酸。符号：L，Leu。 -CMKC端氯甲基酮修饰，Chloromethylketone (CMK) |
| 氨基酸个数: | 4 |
| 分子式: | C35H67O5N10Cl1 |
| 平均分子量: | 743.42 |
| 精确分子量: | 742.5 |
| 等电点(PI): | - |
| pH=7.0时的净电荷数: | 2 |
| 平均亲水性: | 0.6 |
| 疏水性值: | -0.35 |
| 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: | CMK(氯甲基酮)修饰 |
前蛋白转化酶位点1蛋白酶（S1P，也称为枯草杆菌蛋白酶kexin同工酶，SKI-1）的细胞可渗透不可逆抑制剂。Dec-RRLL-CMK有效地阻断了纳摩尔浓度下拉沙病毒糖蛋白前体的加工，尽管观察到的抑制剂的细胞毒性限制了其应用。最初为W.Garten教授合成（2000年4月）。
A cell-permeable irreversible inhibitor of proprotein convertase site 1 protease (S1P, also called subtilisin kexin isozyme, SKI-1). Dec-RRLL-CMK efficiently blocked the processing of Lassa virus glycoprotein precursor at nanomolar concentrations, though the observed cytotoxicity of the inhibitor limits its application. Originally synthesized for Prof. Dr. W. Garten (April 2000).
癸酰‑Arg‑Arg‑Leu‑Leu‑氯甲基酮是一种不可逆抑制剂，用于定位蛋白酶催化几何。其疏水链增强与酶表面亲和力。研究人员通过反应性部分表征共价结合。该分子支持蛋白酶驱动调控通路分析。
Decanoyl-Arg-Arg-Leu-Leu-chloromethylketone is an irreversible inhibitor used to map protease catalytic geometry. Its hydrophobic chain enhances affinity for enzyme surfaces. Researchers study its reactive moiety to characterize covalent binding. The molecule supports analyses of protease-driven regulatory pathways.
| DOI | 名称 | |
|---|---|---|
| 10.1074/jbc.M513675200 | The proprotein convertase SKI-1/S1P. In vitro analysis of Lassa virus glycoprotein-derived substrates and ex vivo validation of irreversible peptide inhibitors | 下载 |
| 10.1371/journal.pntd.0000446 | Inhibition of Lassa virus glycoprotein cleavage and multicycle replication by site 1 protease-adapted alpha(1)-antitrypsin variants | 下载 |
| 10.1128/JVI.01697-09 | Targeting the proteolytic processing of the viral glycoprotein precursor is a promising novel antiviral strategy against arenaviruses | 下载 |
| 10.1074/jbc.M110.151647 | Inhibition of proprotein convertase SKI-1 blocks transcription of key extracellular matrix genes regulating osteoblastic mineralization | 下载 |
| 10.1038/jid.2013.282 | Inhibition of the prohormone convertase subtilisin-kexin isoenzyme-1 induces apoptosis in human melanoma cells | 下载 |
| 10.1016/0300-9084(94)90149-x | Processing of viral glycoproteins by the subtilisin-like endoprotease furin and its inhibition by specific peptidylchloroalkylketones | 下载 |
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