PU02

• 常用名: PU02
• 英文名: PU 02
• CAS号: 313984-77-9
• 分子量: 292.35800
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₆H₁₂N₄S
• 熔点: N/A
• 闪点: N/A

PU02用途

PU02 是 6-MP (HY-13677) 的一个衍生物,是 5-HT3 受体的负变构调节剂,其在 HEK293 细胞测得的转染 5-HT3A 和 5-HT3AB 受体后的 IC50 值分别为 0.36 和 0.73 μM。

PU02名称

• 英文名: 6-[(1-Naphthylmethyl)sulfanyl]-7H-purine

PU02生物活性

• 描述: PU02 是 6-MP (HY-13677) 的一个衍生物,是 5-HT3 受体的负变构调节剂,其在 HEK293 细胞测得的转染 5-HT3A 和 5-HT3AB 受体后的 IC50 值分别为 0.36 和 0.73 μM。
• 相关类别:
  信号通路 >> 细胞凋亡 >> 细胞凋亡
  研究领域 >> 癌症
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
• 靶点实验:

  5-HT3A Receptor:0.36 μM (IC50)

  5-HT 3 AB:0.73 μM (IC50)

• 体外研究: PU02(NMMP)(0-200μM)可使HepG2细胞的存活率持续下降(IC50=48.585μM)。治疗48小时后,PU02(NMMP)对L02细胞的毒性小于6-MP[2]。6.25μM或25μM的PU02(NMMP)对受试细胞系SMMC-7721、MDA-MB-231、RKO和HCT-8细胞的活力具有抑制作用[2]。PU02(NMMP)诱导细胞周期阻滞于G2/M期。PU02(NMMP)对HepG2细胞周期蛋白B1/D1和CDK4的表达呈时间依赖性下调,但不影响cycline的表达[2]。PU02(NMMP)处理的细胞显示出caspase-3裂解的显著增加,表明凋亡活性增强[2]。细胞凋亡分析[2]细胞系：HepG2细胞。浓度：6.26、12.5、25、50μM,孵育时间：6、12、24、36h。结果：诱导线粒体依赖性凋亡。
• 参考文献:

  [1]. Sarah M Trattnig, et al. Discovery of a novel allosteric modulator of 5-HT3 receptors: inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site. J Biol Chem. 2012 Jul 20;287(30):25241-54.

  [2]. Xiao-Guang Yang, et al. 6-[(1-naphthylmethyl)sulfanyl]-9H-purine induces G2/M phase arrest and apoptosis in human hepatocellular carcinoma HepG2 cells. Eur J Pharmacol. 2012 Nov 15;695(1-3):27-33.

PU02物理化学性质

• 分子式: C₁₆H₁₂N₄S
• 分子量: 292.35800
• 精确质量: 292.07800
• PSA: 79.76000
• LogP: 3.79840
• InChIKey: BGMSTNYJYPSLHN-UHFFFAOYSA-N
• SMILES: c1ccc2c(CSc3ncnc4nc[nH]c34)cccc2c1
• 储存条件: -20°C，干燥，密封

PU02安全信息

• 危害码 (欧洲): Xi

PU02靶点实验

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实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

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

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：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：High throughput fluorescence intensity-based biochemical assay to screen for small mo... 来源：University of Pittsburgh Molecular Library Screening Center 靶标：furin (paired basic amino acid cleaving enzyme), isoform CRA_a [Homo sapiens] External Id：MH080376 Biochemical HTS for Inhibitors of the Proprotein Convertase Furin.

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

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：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

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

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PU02英文别名

• MFCD23381174