Leucettine L41

• 常用名: Leucettine L41
• 英文名: Leucettine L41
• CAS号: 1112978-84-3
• 分子量: 307.303
• 密度: 1.4±0.1 g/cm3
• 沸点: N/A
• 分子式: C₁₇H₁₃N₃O₃
• 熔点: N/A
• 闪点: N/A

Leucettine L41用途

亮氨酸L41是双特异性酪氨酸磷酸化调节激酶1A(DYRK1A)、DYRK2、CDC样激酶1(CLK1)和CLK3(IC50s分别为0.04、0.035、0.015和4.5µM)的有效抑制剂[1]。在阿尔茨海默病样毒性小鼠模型中,亮氨酸L41可防止Aβ25-35在海马中诱导的脂质过氧化和活性氧(ROS)积累。亮氨酸L41还可以防止同一模型中Aβ25-35引起的记忆缺陷[2]。

Leucettine L41名称

• 英文名: leucettine L41

Leucettine L41生物活性

• 描述: 亮氨酸L41是双特异性酪氨酸磷酸化调节激酶1A(DYRK1A)、DYRK2、CDC样激酶1(CLK1)和CLK3(IC50s分别为0.04、0.035、0.015和4.5µM)的有效抑制剂[1]。在阿尔茨海默病样毒性小鼠模型中,亮氨酸L41可防止Aβ25-35在海马中诱导的脂质过氧化和活性氧(ROS)积累。亮氨酸L41还可以防止同一模型中Aβ25-35引起的记忆缺陷[2]。
• 相关类别:
  信号通路 >> 蛋白酪氨酸激酶 >> DYRK
  信号通路 >> 细胞周期/DNA损伤 >> CDK
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Debdab M, et al. Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. J Med Chem. 2011 Jun 23;54(12):4172-86.

  [2]. Naert G, et al. Leucettine L41, a DYRK1A-preferential DYRKs/CLKs inhibitor, prevents memory impairments and neurotoxicity induced by oligomeric Aβ25-35 peptide administration in mice. Eur Neuropsychopharmacol. 2015 Nov;25(11):2170-82.

Leucettine L41物理化学性质

• 密度: 1.4±0.1 g/cm3
• 分子式: C₁₇H₁₃N₃O₃
• 分子量: 307.303
• 精确质量: 307.095703
• LogP: 3.49
• 折射率: 1.698

Leucettine L41靶点实验

查看更多实验

实验名称：Inhibition of recombinant human CK1epsilon expressed in Sf9 insect cells incubated fo... 来源：ChEMBL 靶标：Casein kinase I isoform epsilon External Id：CHEMBL5251364

实验名称：Inhibition of DYRK1A in human SH-SY5Y overexpressing Tau4R cells assessed as phosphor... 来源：ChEMBL 靶标：Dual specificity tyrosine-phosphorylation-regulated kinase 1A External Id：CHEMBL5127394

实验名称：Inhibition of recombinant human CDK5/p25 expressed in Sf9 insect cells incubated for ... 来源：ChEMBL 靶标：Cyclin-dependent kinase 5 External Id：CHEMBL5251363

实验名称：Antagonist activity at CP-55940-activated CB1 receptor (unknown origin) at 10 uM by b... 来源：ChEMBL 靶标：Cannabinoid receptor 1 External Id：CHEMBL5127395

实验名称：Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 m... 来源：ChEMBL 靶标：Dual specificity protein kinase CLK2 External Id：CHEMBL5251366

实验名称：Antagonist activity at CP-55940-activated CB1 receptor (unknown origin) by beta-arres... 来源：ChEMBL 靶标：Cannabinoid receptor 1 External Id：CHEMBL5127396

实验名称：Thermal Shift Assay. Domain: start/stop: M1-L298 来源：ChEMBL 靶标：Cyclin-dependent kinase 2 External Id：CHEMBL5062802

实验名称：Inhibition of recombinant human CLK1 expressed in Sf9 insect cells incubated for 60 m... 来源：ChEMBL 靶标：Dual specificity protein kinase CLK1 External Id：CHEMBL5251365

实验名称：Drug metabolism in human liver microsomes assessed as GSH reduction metabolite at 50 ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5127397

实验名称：Neurotoxicity against mouse HT-22 cells assessed as cell survival treated for 24 hrs ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5127390

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Leucettine L41英文别名

• (5Z)-2-Anilino-5-(1,3-benzodioxol-5-ylmethylene)-1,5-dihydro-4H-imidazol-4-one
• leucettine L41