GW5074

GW5074

Catalog Number:
L002369987APE
Mfr. No.:
APE-B1405
Price:
$196
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      • Overview
        • Please contact us at for specific academic pricing.

          Background

          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].
          Our product is a mixture of Z and E configuration.

          [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.

      • Properties
        • Alternative Name
          3-(3,5-dibromo-4-hydroxybenzylidene)-5-iodoindolin-2-one
          CAS Number
          220904-83-6
          Molecular Formula
          C15H8Br2INO2
          Molecular Weight
          520.94
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          insoluble in EtOH; insoluble in H2O; ≥21.9 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Aiste Dobrovolskaite, Meenu Madan, et al. "The discovery of indolone GW5074 during a comprehensive search for non-polyamine-based polyamine transport inhibitors." Int J Biochem Cell Biol. 2021 Sep;138:106038. PMID:34252566

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