Gw5074 3-(3,5-二溴-4-羟基苯亚甲基)-5-碘-1,3-二氢吲哚-2-酮
CAS 220904-83-6 MFCD03453076
化学结构图
SMILES: O=C1Nc2ccc(I)cc2/C1=C/c1cc(Br)c(O)c(Br)c1
化学属性
| Mol. Formula | C15H8Br2INO2 |
|---|---|
| Mol. Weight | 520.94 |
| Appearance | solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | Gw5074 |
|---|---|
| Synonym | 3-(3,5-Dibromo-4-hydroxybenzyliden)-5-iodo-1,3-dihydroindol-2-one GW5074 GW5074; GW 5074; GW-5074; |
| MDL Number | MFCD03453076 |
| PubChem Substance ID | 24278455 |
| CAS Number | 220904-83-6 |
| Chemical Name Translation | 3-(3,5-二溴-4-羟基苯亚甲基)-5-碘-1,3-二氢吲哚-2-酮 |
| Formula | C15H8Br2INO2 |
| IUPAC Name | 3-(3,5-Dibromo-4-hydroxy-benzylidene)-5-iodo-1,3-dihydro-indol-2-one |
| InChIKey | LMXYVLFTZRPNRV-KMKOMSMNSA-N |
| InChI | InChI=1S/C15H8Br2INO2/c16-11-4-7(5-12(17)14(11)20)3-10-9-6-8(18)1-2-13(9)19-15(10)21/h1-6,20H,(H,19,21)/b10-3- |
| Canonical SMILES | O=C1NC2=C(C=C(I)C=C2)/C1=C/C3=CC(Br)=C(O)C(Br)=C3 |
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分类
- {SNA} Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology, Cell Signaling and Neuroscience, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, G, Kinase/Phosphatase Biology,
- {SNA} Bioactive Small Molecule Alphabetical Index, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, G, Kinase/Phosphatase Biology, P to Q, Protein Kinase Inhibitors, Protein Kinase, cRAF1, Raf, Serine/Threonine Kinase Biology, Serine/Threonine Kinase Inhibitors, 生化试剂, 生物活性小分子, 细胞信号转导和神经科学, 细胞生物学, 酶、抑制剂和底物
产品应用
- GW5074 is a c-Raf inhibitor. GW5074 has no direct effect on the activities of several apoptosis-associated kinases when assayed in vitro. In contrast to its effect in vitro, treatment of neurons with GW5074 causes c-Raf activation (when measured in vitro in the absence of the drug) and stimulates the Raf-MEK-ERK pathway. GW5074 prevents neurodegeneration and improves behavioral outcome in an animal model of Huntington's disease. GW5074 could have therapeutic value against neurodegenerative pathologies in humans.
相关文献及参考
- Lackey, K., et al, The discovery of potent cRaf1 kinase inhibitors. Bioorg. Med. Chem. Lett. 10 , 223, (2000) 摘要
- Zhang Q, Adiseshaiah P, Kalvakolanu DV, Reddy SP, A Phosphatidylinositol 3-kinase-regulated Akt-independent signaling promotes cigarette smoke-induced FRA-1 expression. J. Biol. Chem. , 10174-81, (2006) 摘要
- Morrison BE, Majdzadeh N, Zhang X, Lyles A, Bassel-Duby R, Olson EN, D'Mello SR, Neuroprotection by histone deacetylase-related protein. Mol. Cell. Biol. , 3550-64, (2006) 摘要
