GSK PERK抑制剂-d3

• 常用名: GSK PERK抑制剂-d3
• 英文名: PERK-IN-4
• CAS号: 1337531-89-1
• 分子量: 469.434
• 密度: 1.5±0.1 g/cm3
• 沸点: 710.9±60.0 °C at 760 mmHg
• 分子式: C₂₄H₁₉F₄N₅O
• 熔点: N/A
• 闪点: 383.7±32.9 °C

GSK PERK抑制剂-d3用途

PERK-IN-4是一种有效的、选择性的PERK(蛋白激酶R(PKR)样内质网激酶)抑制剂,其ic50为0.3nm。PERK被激活,以应对与多种疾病状态有关的各种内质网应激[1]。

GSK PERK抑制剂-d3名称

• 中文名: GSK PERK抑制剂-d3
• 英文名: 1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-fluoro-5-(trifluoromethyl)phenyl]ethanone

GSK PERK抑制剂-d3生物活性

• 描述: PERK-IN-4是一种有效的、选择性的PERK(蛋白激酶R(PKR)样内质网激酶)抑制剂,其ic50为0.3nm。PERK被激活,以应对与多种疾病状态有关的各种内质网应激[1]。
• 相关类别:
  研究领域 >> 癌症
  研究领域 >> 代谢疾病
  信号通路 >> 细胞周期/DNA损伤 >> PERK
  研究领域 >> 神经疾病
• 靶点实验:

  IC50: 0.3 nM (PERK)[1]

• 参考文献:

  [1]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012;55(16):7193-7207.

GSK PERK抑制剂-d3物理化学性质

• 密度: 1.5±0.1 g/cm3
• 沸点: 710.9±60.0 °C at 760 mmHg
• 分子式: C₂₄H₁₉F₄N₅O
• 分子量: 469.434
• 闪点: 383.7±32.9 °C
• 精确质量: 469.152588
• PSA: 77.04000
• LogP: 4.42
• InChIKey: PXVQGBJMIQCDEX-UHFFFAOYSA-N
• SMILES: Cn1cc(-c2ccc3c(c2)CCN3C(=O)Cc2cc(F)cc(C(F)(F)F)c2)c2c(N)ncnc21
• 蒸汽压: 0.0±2.3 mmHg at 25°C
• 折射率: 1.660

GSK PERK抑制剂-d3靶点实验

查看更多实验

实验名称：Human myosin light chain kinase 2 (Myosin Light Chain Kinase (MLCK) family) 来源：IUPHAR-DB 靶标：myosin light chain kinase 2 (Myosin Light Chain Kinase (MLCK) family) [Homo sapiens] External Id：1553_Human

实验名称：GSK PKIS2: Screen against O. lienalis microfilariae, single point, at 3.1uM to assess... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3988182

实验名称：Human eukaryotic translation initiation factor 2 alpha kinase 3 (PEK subfamily) 来源：IUPHAR-DB 靶标：eukaryotic translation initiation factor 2 alpha kinase 3 (PEK subfamily) [Homo sapiens] External Id：2017_Human

实验名称：Inhibition of NEK9 (unknown origin) at 1 uM relative to control 来源：ChEMBL 靶标：Serine/threonine-protein kinase Nek9 External Id：CHEMBL5252704

实验名称：Inhibition of NEK7 (unknown origin) at 1 uM relative to control 来源：ChEMBL 靶标：Serine/threonine-protein kinase Nek7 External Id：CHEMBL5252703

实验名称：Inhibition of NEK11 (unknown origin) at 1 uM relative to control 来源：ChEMBL 靶标：Serine/threonine-protein kinase Nek11 External Id：CHEMBL5252706

实验名称：Inhibition of NEK10 (unknown origin) at 1 uM relative to control 来源：ChEMBL 靶标：Serine/threonine-protein kinase Nek10 External Id：CHEMBL5252705

实验名称：Inhibition of NEK4 (unknown origin) at 1 uM relative to control 来源：ChEMBL 靶标：Serine/threonine-protein kinase Nek4 External Id：CHEMBL5252700

实验名称：Inhibition of NEK3 (unknown origin) at 1 uM relative to control 来源：ChEMBL 靶标：Serine/threonine-protein kinase Nek3 External Id：CHEMBL5252699

实验名称：Inhibition of NEK6 (unknown origin) at 1 uM relative to control 来源：ChEMBL 靶标：Serine/threonine-protein kinase Nek6 External Id：CHEMBL5252702

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GSK PERK抑制剂-d3英文别名

• 1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoromethyl)phenyl]ethanone
• GSK PERK Inhibitor