(S)-金黄紫堇碱

• 常用名: (S)-金黄紫堇碱
• 英文名: Scoulerine
• CAS号: 6451-73-6
• 分子量: 327.374
• 密度: 1.4±0.1 g/cm3
• 沸点: 503.3±50.0 °C at 760 mmHg
• 分子式: C₁₉H₂₁NO₄
• 熔点: 192ºC
• 闪点: 258.2±30.1 °C

(S)-金黄紫堇碱用途

Scoulerine ((-)-Scoulerine) 是一种有效的抗有丝分裂 (antimitotic) 化合物。Scoulerine 也是 BACE1 (淀粉样前体蛋白裂解酶 1) 的抑制剂。Scoulerine 抑制细胞增殖,阻止细胞周期,并诱导癌细胞凋亡。

(S)-金黄紫堇碱名称

• 中文名: 金黄紫堇碱
• 英文名: (S)-scoulerine

(S)-金黄紫堇碱生物活性

• 描述: Scoulerine ((-)-Scoulerine) 是一种有效的抗有丝分裂 (antimitotic) 化合物。Scoulerine 也是 BACE1 (淀粉样前体蛋白裂解酶 1) 的抑制剂。Scoulerine 抑制细胞增殖,阻止细胞周期,并诱导癌细胞凋亡。
• 相关类别:
  信号通路 >> 细胞凋亡 >> 细胞凋亡
  研究领域 >> 癌症
  信号通路 >> 神经信号通路 >> β-分泌
  信号通路 >> 细胞周期/DNA损伤 >> 微管/微管蛋白
  信号通路 >> 细胞骨架 >> 微管/微管蛋白
• 体外研究: 斯考林((-)-Scoulerine)抑制人类白血病细胞的微型面板,MOLT-4(WT)、Jurkat(TP53突变)、Raji(TP53突变)、HL-60(TP53无效)、U-937(TP53突变)和HEL 92.1.7(野生型),IC50范围从2.7μM到6.5μM[1]。斯考林(2.5-20μM；24小时)可减少Jurkat和MOLT-4细胞的增殖[1]。斯考林(2.5-20μM；24小时)诱导MOLT-4和Jurkat细胞凋亡[1]。斯考林诱导G2或M细胞周期阻滞[1]。斯考林(2.5-5μM；24小时)显示p53野生型MOLT-4细胞中p53蛋白上调[1]。斯考林(2.5-5μM；24-48小时)以剂量依赖性方式激活caspase-3/7、-8和-9[1]。司洛林(5-10µM；24小时)破坏A549肺癌细胞微管结构[1]细胞增殖试验[1]细胞系：Jurkat和MOLT-4细胞浓度：2.5、5、10、15和20μM孵育时间：24小时结果：显著降低Jurkat和MOLT-4细胞的活性和增殖,呈剂量依赖性。细胞凋亡分析[1]细胞系：MOLT-4和Jurkat细胞浓度：2.5,5,10,15,20μM孵育时间：24小时结果：诱导MOLT-4和Jurkat细胞凋亡。细胞周期分析[1]细胞系：Jurkat和MOLT-4白血病细胞浓度：2.5-20µM孵育时间：16小时结果：诱导细胞周期停滞在G2/M过渡期。Western Blot分析[1]细胞系：MOLT-4细胞浓度：2.5,5μM孵育时间：24小时结果：野生型MOLT-4细胞p53蛋白表达上调。
• 参考文献:

  [1]. Habartova K, et al. Scoulerine affects microtubule structure, inhibits proliferation, arrests cell cycle and thus culminates in the apoptotic death of cancer cells. Sci Rep. 2018;8(1):4829. Published 2018 Mar 19.

(S)-金黄紫堇碱物理化学性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 503.3±50.0 °C at 760 mmHg
• 熔点: 192ºC
• 分子式: C₁₉H₂₁NO₄
• 分子量: 327.374
• 闪点: 258.2±30.1 °C
• 精确质量: 327.147064
• PSA: 62.16000
• LogP: 2.16
• InChIKey: KNWVMRVOBAFFMH-HNNXBMFYSA-N
• SMILES: COc1cc2c(cc1O)C1Cc3ccc(OC)c(O)c3CN1CC2
• 蒸汽压: 0.0±1.3 mmHg at 25°C
• 折射率: 1.680
• 储存条件: -20°C，干燥，密封

(S)-金黄紫堇碱毒性和生态

(S)-金黄紫堇碱安全信息

• 危害码 (欧洲): Xi

(S)-金黄紫堇碱靶点实验

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实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

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实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

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实验名称：GPR151 activator identification: cell-based high-throughput confirmation assay 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_3X%ACT CRUN1

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(S)-金黄紫堇碱英文别名

• 2,9-DIOXY-3,10-DIMETHOXYBERBINE
• (±)-Scoulerine
• 3,10-Dimethoxy-5,8,13,13a-tetrahydro-6H-isoquinolino[3,2-a]isoquinoline-2,9-diol
• Scoulerin
• Aequaline
• Alkaloid HF-1
• l-scoulerine
• (RS)-Scoulerine
• scoulerine
• l-skoulerine