Home MAPK Raf inhibitor - Apoptosis related inhibitor GW5074 For research use only.

GW5074

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. GW5074 inhibits LK-induced apoptosis.

GW5074 Chemical Structure

GW5074 Chemical Structure

CAS: 220904-83-6

Selleck's GW5074 has been cited by 25 Publications

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Purity & Quality Control

Batch: S287201 DMSO] 104 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.8%
99.8

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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. GW5074 inhibits LK-induced apoptosis.
Targets
C-Raf [1]
(Cell-free assay)
9 nM
In vitro
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]
Kinase Assay 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 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Raf-1 / Raf-1 / p-c-Jun / c-Junc / c-Fos / P-gp 28212576
In Vivo
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 suppresses sidestream smoke-induced airway hyperresponsiveness in mice. [3]
Animal Research Animal Models Eight-week-old C57BL/6 male mice administered with 50–55 mg/kg 3-NP
Dosages 0.5–10 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 520.94 Formula

C15H8Br2INO2
CAS No. 220904-83-6 SDF Download GW5074 SDF
Smiles C1=CC2=C(C=C1I)C(=CC3=CC(=C(C(=C3)Br)O)Br)C(=O)N2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 104 mg/mL ( (199.63 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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