GSK690

• 常用名: GSK690
• 英文名: GSK690
• CAS号: 2101305-84-2
• 分子量: 369.459
• 密度: 1.2±0.1 g/cm3
• 沸点: 530.5±50.0 °C at 760 mmHg
• 分子式: C₂₄H₂₃N₃O
• 熔点: N/A
• 闪点: 274.6±30.1 °C

GSK690用途

GSK 690是赖氨酸特异性脱甲基酶1(LSD1)的可逆抑制剂,Kd值为9 nM,生化IC50为37 nM。

GSK690名称

• 英文名: 4-{2-(4-Methylphenyl)-5-[(3R)-3-pyrrolidinylmethoxy]-3-pyridinyl}benzonitrile

GSK690生物活性

• 描述: GSK 690是赖氨酸特异性脱甲基酶1(LSD1)的可逆抑制剂,Kd值为9 nM,生化IC50为37 nM。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 表观遗传学 >> 组蛋白去甲基化酶
• 体外研究: GSK690(1-10μM)与JNJ-26481585一起作用,在所有四种受试RMS细胞系(RD、RH30、RMS13和TE381.T细胞)中诱导细胞死亡[2]。GSK690/JNJ-26481585共处理改变了促凋亡蛋白和抗凋亡蛋白之间的平衡,1 用于RD电池的μM GSK690)和10 μM GSK690用于RH30细胞[2]。GSK690/JNJ-26481585共处理诱导caspase依赖性细胞死亡 用于RD电池的μM GSK690和10 μM GSK690用于RH30细胞[2]。GSK690的加入进一步增强了JNJ-26481585刺激的G2/M阻滞[2]。
• 参考文献:

  [1]. Mould DP, et al. Development of (4-Cyanophenyl)glycine Derivatives as Reversible Inhibitors of Lysine Specific Demethylase 1. J Med Chem. 2017 Oct 12;60(19):7984-7999.

  [2]. Haydn T, et al. Concomitant epigenetic targeting of LSD1 and HDAC synergistically induces mitochondrial apoptosis in rhabdomyosarcoma cells. Cell Death Dis. 2017 Jun 15;8(6):e2879.

GSK690物理化学性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 530.5±50.0 °C at 760 mmHg
• 分子式: C₂₄H₂₃N₃O
• 分子量: 369.459
• 闪点: 274.6±30.1 °C
• 精确质量: 369.184113
• LogP: 3.75
• InChIKey: IQVDLEXWAPYWDT-LJQANCHMSA-N
• SMILES: Cc1ccc(-c2ncc(OCC3CCNC3)cc2-c2ccc(C#N)cc2)cc1
• 蒸汽压: 0.0±1.4 mmHg at 25°C
• 折射率: 1.640

GSK690靶点实验

查看更多实验

实验名称：Inhibition of MAO-A (unknown origin) assessed as oxidative deamination of kynuramine ... 来源：ChEMBL 靶标：Amine oxidase [flavin-containing] A External Id：CHEMBL3135141

实验名称：Inhibition of LSD1 (unknown origin) using histone H3 (1 to 21) K4(Me1)-biotin peptide... 来源：ChEMBL 靶标：Lysine-specific histone demethylase 1A External Id：CHEMBL3135142

实验名称：Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibit... 来源：ChEMBL 靶标：MV4-11 External Id：CHEMBL5370465

实验名称：Antiproliferative activity against human NCI-H1417 cells assessed as cell growth inhi... 来源：ChEMBL 靶标：NCI-H1417 External Id：CHEMBL5370466

实验名称：Inhibition of human recombinant LSD1 expressed in Escherichia coli using H3K4me2 pept... 来源：ChEMBL 靶标：Lysine-specific histone demethylase 1A External Id：CHEMBL5370463

实验名称：Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibi... 来源：ChEMBL 靶标：MOLM-13 External Id：CHEMBL5370464

实验名称：Inhibition of human ERG at 10 uM relative to control 来源：ChEMBL 靶标：Potassium voltage-gated channel subfamily H member 2 External Id：CHEMBL4310495

实验名称：Inhibition of LSD1 in human THP1 cells assessed as induction of CD11b expression afte... 来源：ChEMBL 靶标：Lysine-specific histone demethylase 1A External Id：CHEMBL4310494

实验名称：Inhibition of LSD1 (unknown origin) 来源：ChEMBL 靶标：Lysine-specific histone demethylase 1A External Id：CHEMBL4310493

实验名称：Binding affinity to human LSD1/CoREST assessed as dissociation constant by competitiv... 来源：ChEMBL 靶标：REST corepressor 1 External Id：CHEMBL5123803

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GSK690英文别名

• 4-{2-(4-Methylphenyl)-5-[(3R)-3-pyrrolidinylmethoxy]-3-pyridinyl}benzonitrile