LSD1-IN-20

• 常用名: LSD1-IN-20
• 英文名: LSD1-IN-20
• CAS号: 1239589-91-3
• 分子量: 478.63
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₇H₃₈N₆O₂
• 熔点: N/A
• 闪点: N/A

LSD1-IN-20用途

LSD1-IN-20(化合物1)是一种有效的双非共价LSD1/G9a抑制剂,Ki值分别为0.44和0.68μM。LSD1-IN-20在THP-1白血病细胞和MDA-MB-231乳腺癌细胞中显示出抗增殖活性,IC50(72小时)分别为0.51和1.60μM【1】。

LSD1-IN-20名称

• 英文名: LSD1-IN-20

LSD1-IN-20生物活性

• 描述: LSD1-IN-20(化合物1)是一种有效的双非共价LSD1/G9a抑制剂,Ki值分别为0.44和0.68μM。LSD1-IN-20在THP-1白血病细胞和MDA-MB-231乳腺癌细胞中显示出抗增殖活性,IC50(72小时)分别为0.51和1.60μM【1】。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 表观遗传学 >> 组蛋白甲基转移酶
  信号通路 >> 表观遗传学 >> 组蛋白去甲基化酶
• 靶点实验:

  Ki of 0.440 ± 0.05 μM (LSD1), 0.68 ± 0.02 μM (G9a)[1]

• 参考文献:

  [1]. Menna M, et al. Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models. Eur J Med Chem. 2022 Jul 5;237:114410.

LSD1-IN-20物理化学性质

• 分子式: C₂₇H₃₈N₆O₂
• 分子量: 478.63

LSD1-IN-20靶点实验

查看更多实验

实验名称：Antiproliferative activity against human THP-1 cells assessed as inhibition of cell g... 来源：ChEMBL 靶标：THP-1 External Id：CHEMBL5123819

实验名称：Antiproliferative activity against human THP-1 cells assessed as inhibition of cell g... 来源：ChEMBL 靶标：THP-1 External Id：CHEMBL5123820

实验名称：Antiproliferative activity against human THP-1 cells assessed as inhibition of cell g... 来源：ChEMBL 靶标：THP-1 External Id：CHEMBL5123818

实验名称：Binding affinity to LSD1 (unknown origin) assessed as change in melting temperature b... 来源：ChEMBL 靶标：Lysine-specific histone demethylase 1A External Id：CHEMBL5241952

实验名称：Inhibition of human LSD1 (unknown orgin) 来源：ChEMBL 靶标：Lysine-specific histone demethylase 1A External Id：CHEMBL5241943

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

实验名称：Inhibition of human LSD1/CoREST using histone H3 peptide as substrate by fluorescence... 来源：ChEMBL 靶标：REST corepressor 1 External Id：CHEMBL5123804

实验名称：Inhibition of G9a (unknown origin) assessed as reduction in substrate methylation usi... 来源：ChEMBL 靶标：Histone-lysine N-methyltransferase EHMT2 External Id：CHEMBL5123805

实验名称：Inhibition of human G9a using biotinylated peptide H3( 1 to 25 residues) as substrate... 来源：ChEMBL 靶标：Histone-lysine N-methyltransferase EHMT2 External Id：CHEMBL4262303

实验名称：Antiplasmodial activity against Plasmodium falciparum 3D7 after 3 days by SYBR green1... 来源：ChEMBL 靶标：Plasmodium falciparum External Id：CHEMBL4262302

共28条，当前第1页，共3页

1

2

3