Leucettinib-92

• 常用名: Leucettinib-92
• 英文名: Leucettinib-92
• CAS号: 2732859-57-1
• 分子量: 378.49
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₁H₂₂N₄OS
• 熔点: N/A
• 闪点: N/A

Leucettinib-92用途

Leucettinib-92 (compound 92) 是 DYRK/CLK 激酶的抑制剂,IC50s 分别为 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3)。

Leucettinib-92名称

• 英文名: Leucettinib-92

Leucettinib-92生物活性

• 描述: Leucettinib-92 (compound 92) 是 DYRK/CLK 激酶的抑制剂,IC50s 分别为 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3)。
• 相关类别:
  信号通路 >> 蛋白酪氨酸激酶 >> DYRK
  研究领域 >> 其他
  信号通路 >> 细胞周期/DNA损伤 >> CDK
• 靶点实验:

  IC50: 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3)[1]

• 参考文献:

  [1]. Deau E, et al. Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B. J Med Chem. 2023 Aug 10;66(15):10694-10714.

Leucettinib-92物理化学性质

• 分子式: C₂₁H₂₂N₄OS
• 分子量: 378.49
• InChIKey: HEVBCYZPXGZFGS-FMQZQXMHSA-N
• SMILES: O=C1NC(=NC23CC4CC(CC(C4)C2)C3)NC1=Cc1ccc2ncsc2c1

Leucettinib-92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 human full-length recombinant DYRK1A using RRRFRPASPLRGPPK and [gamma33... 来源：ChEMBL 靶标：Dual specificity tyrosine-phosphorylation-regulated kinase 1A External Id：CHEMBL5363966

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：Inhibition of human full-length recombinant DYRK1B using RRRFRPASPLRGPPK and [gamma33... 来源：ChEMBL 靶标：Dual specificity tyrosine-phosphorylation-regulated kinase 1B External Id：CHEMBL5363967

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：Inhibition of human CIT using KKLRRTLSVA and [gamma33P]ATP as substrate at 0.1 uM inc... 来源：ChEMBL 靶标：Citron Rho-interacting kinase External Id：CHEMBL5363964

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：Inhibition of human recombinant CLK2 (138 to end residues) using YRRAAVPPSPSLSRHSSPHQ... 来源：ChEMBL 靶标：Dual specificity protein kinase CLK2 External Id：CHEMBL5363965

实验名称：Thermal Shift Assay. Domain: start/stop: S229-K512 来源：ChEMBL 靶标：Tyrosine-protein kinase ABL1 External Id：CHEMBL5060747

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