GW5074

Catalog No.S2872

GW5074 Chemical Structure

Molecular Weight(MW): 520.94

GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted.

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4 Customer Reviews

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    Effect of select kinase inhibitors on DF508-CFTR maturation analyzed by immunoblotting. 293MSR-GT cells stably expressing DF508-CFTR were treated with 15 uM kinase inhibitors or 0.3% DMSO (vehicle control), as indicated, grown at 37 °C for 48 h, and the appearance of the mature protein, band C, monitored by immunoblotting with anti-CFTR antibodies. Band B represents the immature protein. DMSO represents vehicle-alone control, 27 °C represents  temperature rescue of F508-CFTR at 27 °C, 37 °C represents untreated DF508-CFTR control, and WT represents WT-CFTR. Top panels depict the anti-CFTR immunoblot and bottom panels depict actin (loading) control. ** represents cellular toxicity.

     

    Mol Cell Proteomics 2012 11, 745-57. GW5074 purchased from Selleck.

    Effect of kinase inhibitors on cell surface expression of DF508-CFTR analyzed by flow cytometry. Summary of increase in cell surface expression of DF508-CFTR (% change in fluorescence intensity) of the hits analyzed by flow cytometry (two independent experiments, 10,000 live cells per treatment per experiment).

    Mol Cell Proteomics 2012 11, 745-57. GW5074 purchased from Selleck.

  • (I,J) Pretreatment with the C-Raf inhibitor GW5074 (5 μmol/L) abolished the protective efficacy of nesfatin-1 (10−9 mol/L) on the MPP+-induced collapse of the ΔΨm. (K,L) Pretreatment with GW5074 (5 μmol/L) abolished the protective effect of nesfatin-1 (10−9 mol/L) on caspase-3 activation induced by MPP+. *P < 0.05 compared with the control group. #P < 0.05 compared with the MPP+-treated group.

    Sci Rep, 2017, 7:40961. GW5074 purchased from Selleck.

    F. Cell viability of VemR A375 melanoma cells treated with gefitinib, linsitinib, GW5074 individually or in different combination with 2 uM vemurafenib for 72 hrs. G. The expression levels of p-ERK and p-AKT proteins of VemR A375 melanoma cells treated with gefitinib, linsitinib, GW5074 individually or in different combination with 2 uM vemurafenib for 72 hrs. These experiments were carried out in triplicate and results are shown as the mean ± SD. *p < 0.05, **p < 0.01.

    Oncotarget, 2016, 7(33):53558-53570. GW5074 purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted.
Targets
C-Raf [1]
(Cell-free assay)
9 nM
In vitro

GW5074 is a potent and specific inhibitor of c-Raf with IC50 of 9 nM and has no effect of MKK6, MKK7, p38 MAP kinase and cdks in vitro. However, treatment of neuronal cultures with GW5074 permits accumulation of activating modifications on c-Raf and also B-Raf. The inhibition of LK-induced apoptosis by GW5074 in cerebellar granule neurons is not MEK-ERK-dependent. GW5074 delays down-regulation of Akt activity but inhibits apoptosis by an Akt-independent mechanism. GW5074 affects Ras, nuclear factor-kappa B and c-jun. GW5074 inhibits cell death caused by neurotoxins in granule cells and other neuronal types. [1]

In vivo GW5074 is protective in an in vivo experimental model of Huntington’s disease. GW5074 (5 mg/Kg) completely prevented extensive bilateral striatal lesions induced by 3-NP in mice. [1] GW5074 completely abolishes chronic morphine-mediated AC superactivation I in CHO cells stably expressing the humanμ-opioid receptor. [2] GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice. [3]

Protocol

Kinase Assay:[1]
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Affinity determination:

In general, in vitro kinase assays are performed using purified kinase and synthetic substrates under standard conditions using the Kinase Profiling service of Upstate Biotechnology. Briefly, for each assay 5–10 mU of purified kinase is used. For GSK3β, cdk1, cdk2, cdk3, cdk5, the kinase is incubated with 1 μM GW5074 in a buffer containing 8 mM MOPS, pH 7.2, 0.2 mM EDTA, 10 mM magnesium acetate and [c- 33P-ATP] for 40 min at room temperature. Kinase activity is quantified by measuring 33P incorporation by spotting an aliquot on P30 filters, washing in 50 mM phosphoric acid and scintillation counting. The buffer composition for c-Raf, JNK1, JNK2, JNK3, MEK1, MKK6, MKK7 is 50 mM Tris pH 7.5, 0.1 mM EGTA, 10 mM magnesium acetate and [c- 33P-ATP]. The peptide substrates used are as follows: For c-Raf, 0.66 mg/mL MBP; for cdks, 0.1 mg/mL histone H1; for JNKs, 3 μM ATF2; for MEK1, 1 μM MAPK2; for MKK6, 1 μM of SAPK2a and for MKK7, 2 μM JNK1α.
Cell Research:[1]
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  • Cell lines: Cortical neurons
  • Concentrations: ~5 μM
  • Incubation Time: 24 hours
  • Method: HCA is diluted from 100-fold concentrated solutions that are adjusted to pH 7.5. To evaluate the effects of GW5074 on HCA-induced cytotoxicity, GW5074 is added at the time cortical neurons are exposed to HCA. Viability is assessed 24 h later.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Eight-week-old C57BL/6 male mice administered with 50–55 mg/kg 3-NP
  • Formulation: In saline
  • Dosages: 0.5–10 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 104 mg/mL (199.63 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 520.94
Formula

C15H8Br2INO2

CAS No. 220904-83-6
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Raf Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID