ThioLox

• 常用名: ThioLox
• 英文名: ThioLox
• CAS号: 1202193-89-2
• 分子量: 274.38
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₅H₁₈N₂OS
• 熔点: N/A
• 闪点: N/A

ThioLox用途

ThioLox是一种竞争性15-脂氧合酶-1(15-LOX-1)抑制剂,Ki为3.30μM。ThioLox具有抗炎和神经保护财产[1]。

ThioLox名称

• 英文名: ThioLox

ThioLox生物活性

• 描述: ThioLox是一种竞争性15-脂氧合酶-1(15-LOX-1)抑制剂,Ki为3.30μM。ThioLox具有抗炎和神经保护财产[1]。
• 相关类别:
  研究领域 >> 炎症/免疫
  信号通路 >> 代谢酶/蛋白酶 >> 5脂氧合酶
  研究领域 >> 神经疾病
• 靶点实验:

  Ki: 3.30 μM (15-LOX-1)[1]

• 体外研究: ThioLox(50μM；24小时)抑制精确切肺切片 (百分比)中白细胞介素 (IL-1β、IL-6、IL-8、IL-12b、TNFα和 iNOS)的表达[1]。 ThioLox(10μM；16小时)在神经元细胞中防止脂质过氧化和线粒体超氧化物的形成[1]。 ThioLox(5-20μM；14-16小时)保护 HT-22型细胞免受谷氨酸毒性,显著降低神经元细胞死亡[1]。 RT-PCR[1]细胞系：精确切割肺切片(PCLS)浓度：1、5、10、25和50μM培养时间：与10μM亚油酸组合20小时,并用10 ng/mL LPS刺激最后4小时。结果：在50μM时,对促炎基因IL-1β、IL-6、IL-8、IL-12b、TNFα和iNOS的表达提供了几乎50%的抑制。细胞活力测定[1]细胞系：神经元HT-22细胞浓度：5、10和20μM培养时间：14-16小时结果：显著降低了神经元细胞对谷氨酸毒性的死亡。
• 体内研究: ThioLox公司的 对数P值为 3.测得的数值预测能透过血脑屏障[1]。
• 参考文献:

  [1]. Eleftheriadis N, et al. Design of a novel thiophene inhibitor of 15-lipoxygenase-1 with both anti-inflammatory and neuroprotective properties. Eur J Med Chem. 2016 Oct 21;122:786-801.

ThioLox物理化学性质

• 分子式: C₁₅H₁₈N₂OS
• 分子量: 274.38
• InChIKey: QWWMJRJCSZMXHZ-UHFFFAOYSA-N
• SMILES: CCCCNC(=O)c1cc(-c2ccccc2)sc1N
• 外观性状: 固体
• 储存条件: 2-8°C

ThioLox靶点实验

查看更多实验

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in... 来源：NCGC 靶标：TDP1 protein [Homo sapiens] External Id：TDP1100

实验名称：qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in... 来源：NCGC 靶标：TDP1 protein [Homo sapiens] External Id：TDP1101

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

实验名称：qHTS for Inhibitors of AMA1-RON; Towards Development of Antimalarial Drug Lead: Prima... 来源：NCGC 靶标：apical membrane antigen 1, AMA1 [Plasmodium falciparum 3D7] External Id：AMA1100

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：abhydrolase domain-containing protein 4 isoform 1 [Mus musculus] External Id：ABHD4_INH_FP_1536_1X%INH PRUN

实验名称：Identification of agents that induce E-selectin on human endothelial cells Measured i... 来源：Broad Institute 靶标：E-Selectin External Id：2152-01_Activator_SinglePoint_HTS_Activity

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

实验名称：VEID(2) R110 Enzymatic Primary HTS to identify Inhibitors of Caspase 6 Measured in Bi... 来源：Broad Institute 靶标：Caspase 6, apoptosis related cysteine peptidase External Id：7052-01_Inhibitor_SinglePoint_HTS_Activity_Set2

实验名称：Counterscreen for inhibitors of 5-meCpG-binding domain protein 2 (MBD2): TRFRET-based... 来源：The Scripps Research Institute Molecular Screening Center 靶标：E3 ubiquitin-protein ligase UHRF1 isoform 1 [Homo sapiens] External Id：UHRF1-CPGDNA_INH_TRFRET_1536_1X%INH CSRUN for MBD2-CPGDNA INH

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