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GW 5074
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C15H8Br2INO2
- MW: 520.94
Description
Potent, brain-permeable inhibitor of c-Raf (IC50 value 9 nM) when tested in vitro with no effect on the activities of CDK1/2/5/6, JNK1/2/3, c-Src, MEK1, p38 MAP kinase, VEGFR2, and c-fms. In contrast to its effect in vitro, treatment of neurons with GW 5074 causes c-Raf activation (when measured in vitro inthe absence of the drug) and stimulates the Raf-MEK-ERK pathway. GW 5074 protects neurons from death in culture and in an in vivo paradigm of neurodegeneration.
More Information
| Parent CAS No. | 220904-83-6 |
|---|---|
| Chemical Name | 3-(3,5-dibromo-4-hydroxybenzylidene)-5-iodoindolin-2-one |
| SMILES | N1C2=C(C=C(I)C=C2)/C(=C/C2=CC(Br)=C(O)C(Br)=C2)/C1=O |
| MFCD | MFCD03453076 |
| 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- |
| InChiKey | LMXYVLFTZRPNRV-KMKOMSMNSA-N |
| CID | 5924208 |
| Short Description | C-Raf inhibitor |
References
- PC Chin et al. The c-Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK-ERK and Akt-independent mechanism. J Neurochem. 2004 Aug;90(3):595-608.
- K. Lackey et al. The discovery of potent cRaf1 kinase inhibitors. Bioorg Med Chem Lett. 2000 Feb 7;10(3):223-6.
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