GW5074 |
| رقم الكتالوجGC11685 |
GW5074 هو مثبط c-Raf فعال وانتقائي مع IC50 من 9 نانومتر ، وليس له أي تأثير على أنشطة JNK1 / 2/3 أو MEK1 أو MKK6 / 7 أو CDK1 / 2 أو c-Src أو p38 MAP أو VEGFR2 أو c -Fms.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 220904-83-6
Sample solution is provided at 25 µL, 10mM.
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GW5074 is a synthetic inhibitor of c-Raf with IC50 value of 9nM [1].
GW5074 is found to be a potent inhibitor of c-Raf and has no effect on cdk1, cdk2, c-src, p38 MAP kinase, VEGFR2 and c-fms. GW5074 also shows no direct effect on JNK proteins and p38 MAP kinase. In neurons, GW5074 reduces the phosphorylation level of c-Raf at Ser259, results in an induction of c-Raf activity. It is further proved that GW5074 shows neuroprotective efficacy when its dose is below 1μM. In addition, GW5074 suppresses cell apoptosis through delaying the down-regulation of Akt phosphorylation and preventing the activation of GSK3β. In the in vivo model of Huntington’s disease, GW5074 protects neurons via resisting 3-NP-induced striatal neurodegeneration [1].
References:
[1] Burgess S, Echeverria V. Raf inhibitors as therapeutic agents against neurodegenerative diseases. CNS & Neurological Disorders-Drug Targets (Formerly Current Drug Targets-CNS & Neurological Disorders), 2010, 9(1): 120-127.
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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