PBD-150

• 常用名: PBD-150
• 英文名: PBD-150
• CAS号: 790663-33-1
• 分子量: 320.411
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₅H₂₀N₄O₂S
• 熔点: N/A
• 闪点: N/A

PBD-150用途

一种有效的谷氨酰胺环化酶(QC)抑制剂,Ki为60 nM；显着减少转基因小鼠模型和阿尔茨海默病果蝇模型中脑中Aβ3(pGlu)-40/42的沉积。

PBD-150名称

• 中文名: 1-(3-(1H-咪唑-1-基)丙基)-3-(3,4-二甲氧基苯基)硫脲
• 英文名: PBD-150

PBD-150生物活性

• 描述: 一种有效的谷氨酰胺环化酶(QC)抑制剂,Ki为60 nM；显着减少转基因小鼠模型和阿尔茨海默病果蝇模型中脑中Aβ3(pGlu)-40/42的沉积。
• 相关类别:
  研究领域 >> 神经疾病
• 体内研究: PBD-150能够减少Alzheimer病转基因小鼠脑内焦谷氨酸修饰的淀粉样β肽的沉积,从而显著改善这些转基因动物的学习记忆[3]。
• 参考文献:

  [1]. Buchholz M, et al. The first potent inhibitors for human glutaminyl cyclase: synthesis and structure-activity relationship. J Med Chem. 2006 Jan 26;49(2):664-77.

  [2]. DiPisa F, et al. The soluble Y115E-Y117E variant of human glutaminyl cyclase is a valid target for X-ray and NMR screening of inhibitors against Alzheimer disease. Acta Crystallogr F Struct Biol Commun. 2015 Aug;71(Pt 8):986-92.

  [3]. Huang KF, et al. Structures of human Golgi-resident glutaminyl cyclase and its complexes with inhibitors reveal a large loop movement upon inhibitor binding. J Biol Chem. 2011 Apr 8;286(14):12439-49.

PBD-150物理化学性质

• 分子式: C₁₅H₂₀N₄O₂S
• 分子量: 320.411
• InChIKey: FZQXMGLQANXZRP-UHFFFAOYSA-N
• SMILES: COc1ccc(NC(=S)NCCCn2ccnc2)cc1OC
• 储存条件: 2-8°C， 密封， 干燥

PBD-150靶点实验

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实验名称：Inhibitor Assay from Article 10.1074/jbc.M110.208595: "Structures of human Golgi-resi... 来源：BindingDB 靶标：N/A External Id：BindingDB_5650_1

实验名称：Inhibition of human glutaminyl cyclase expressed in Pichia pastoris by pGAP coupled e... 来源：ChEMBL 靶标：Glutaminyl-peptide cyclotransferase External Id：CHEMBL1057686

实验名称：Effective permeability of the compound at 100 ug/ml after 4 hrs by PAMPA 来源：ChEMBL 靶标：N/A External Id：CHEMBL4014212

实验名称：Experimentally measured binding affinity data (Ki) for protein-ligand complexes deriv... 来源：Shanghai Institute of Organic Chemistry 靶标：N/A External Id：PDBbind-Ki for protein-ligand complexes

实验名称：Inhibition of human glutaminyl cyclase overexpressed in HEK293 cells coexpressing amy... 来源：ChEMBL 靶标：Glutaminyl-peptide cyclotransferase External Id：CHEMBL1057687

实验名称：Binding affinity to sQC (unknown origin) assessed as inhibition constant 来源：ChEMBL 靶标：Glutaminyl-peptide cyclotransferase External Id：CHEMBL5512195

实验名称：Inhibition of N-terminal his6-tagged human recombinant glutaminyl cyclase expressed i... 来源：ChEMBL 靶标：Glutaminyl-peptide cyclotransferase External Id：CHEMBL5358516

实验名称：QC Inhibition Testing from Article 10.1021/jm050756e: "The first potent inhibitors fo... 来源：BindingDB 靶标：N/A External Id：BindingDB_993_1

实验名称：Inhibition of human recombinant glutaminyl cyclase expressed in Escherichia coli usin... 来源：ChEMBL 靶标：Glutaminyl-peptide cyclotransferase External Id：CHEMBL3784463

实验名称：Inhibition of recombinant human isoQC using H-Gln-AMC hydrobromide as fluorogenic sub... 来源：ChEMBL 靶标：Glutaminyl-peptide cyclotransferase-like protein External Id：CHEMBL5149904

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