MLS000544460

• 常用名: MLS000544460
• 英文名: MLS000544460
• CAS号: 352336-36-8
• 分子量: 341.36
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₇H₁₂FN₃O₂S
• 熔点: N/A
• 闪点: N/A

MLS000544460用途

MLS000544460 是一种高度选择性和可逆的 Eya2 磷酸酶抑制剂,Kd 为 2.0 μM,IC50 为 4 μM。MLS000544460 抑制 Eya2 磷酸酶介导的细胞迁移,并具有抗癌活性。

MLS000544460名称

• 英文名: MLS000544460

MLS000544460生物活性

• 描述: MLS000544460 是一种高度选择性和可逆的 Eya2 磷酸酶抑制剂,Kd 为 2.0 μM,IC50 为 4 μM。MLS000544460 抑制 Eya2 磷酸酶介导的细胞迁移,并具有抗癌活性。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 代谢酶/蛋白酶 >> 磷酸酶
• 靶点实验:

  Kd: 2.0 μM (Eya2 phosphatase)[1] IC50: 4 μM (Eya2 phosphatase)[1]

• 体外研究: MLS000544460不结合Eya3磷酸酶(ED)[1]。MLS000544460(10μM)抑制Eya2介导的人Eya2细胞迁移,Eya2磷酸酶死亡(D274N)和YFP(作为阴性对照)表达MCF10A细胞[1]。当Eya2ED被透析成10μM EDTA以除去Mg2+时,它以更高的亲和力(Kd=0.80μM)结合MLS000544460,表明这类化合物与Eya2ED的相互作用不需要Mg2+。
• 参考文献:

  [1]. Krueger AB, et al. Allosteric inhibitors of the Eya2 phosphatase are selective and inhibit Eya2-mediated cellmigration. J Biol Chem. 2014 Jun 6;289(23):16349-61.

MLS000544460物理化学性质

• 分子式: C₁₇H₁₂FN₃O₂S
• 分子量: 341.36
• InChIKey: VDKNIVFIPSLUFD-RGVLZGJSSA-N
• SMILES: O=C(NN=Cc1ccc(Sc2ccccn2)o1)c1cccc(F)c1
• 储存条件: 2-8°C，干燥，密封

MLS000544460安全信息

• 危害码 (欧洲): Xi

MLS000544460靶点实验

查看更多实验

实验名称：Inhibition of GST-fused human Eya2 ED (253 to 538 residues) expressed in Escherichia ... 来源：ChEMBL 靶标：Eyes absent homolog 2 External Id：CHEMBL4422542

实验名称：Reversible inhibition of GST-fused human Eya2 ED (253 to 538 residues) expressed in E... 来源：ChEMBL 靶标：Eyes absent homolog 2 External Id：CHEMBL4422562

实验名称：Mixed type inhibition of GST-fused human Eya2 ED (253 to 538 residues) expressed in E... 来源：ChEMBL 靶标：Eyes absent homolog 2 External Id：CHEMBL4422563

实验名称：Mixed type inhibition of GST-fused human Eya2 ED (253 to 538 residues) expressed in E... 来源：ChEMBL 靶标：Eyes absent homolog 2 External Id：CHEMBL4422564

实验名称：Mixed type inhibition of GST-fused human Eya2 ED (253 to 538 residues) expressed in E... 来源：ChEMBL 靶标：Eyes absent homolog 2 External Id：CHEMBL4422565

实验名称：Mixed type inhibition of GST-fused human Eya2 ED (253 to 538 residues) expressed in E... 来源：ChEMBL 靶标：Eyes absent homolog 2 External Id：CHEMBL4422566

实验名称：Mixed type inhibition of GST-fused human Eya2 ED (253 to 538 residues) expressed in E... 来源：ChEMBL 靶标：Eyes absent homolog 2 External Id：CHEMBL4422567

实验名称：Binding affinity to GST-fused human Eya2 ED (253 to 538 residues) expressed in Escher... 来源：ChEMBL 靶标：Eyes absent homolog 2 External Id：CHEMBL4422554

实验名称：Binding affinity to GST-fused human Eya2 ED (253 to 538 residues) expressed in Escher... 来源：ChEMBL 靶标：Eyes absent homolog 2 External Id：CHEMBL4422555

实验名称：Binding affinity to Mg2+ ion at 25 uM in aqueous buffers by UV spectroscopy 来源：ChEMBL 靶标：N/A External Id：CHEMBL4422556

共20条，当前第1页，共2页

1

2