GW5074 Chemical Properties

Boiling point:

561.4±50.0 °C(Predicted)

Density 

2.248±0.06 g/cm3(Predicted)

storage temp. 

room temp

solubility 

DMSO: soluble

pka

5.86±0.25(Predicted)

form 

solid

color 

yellow to orange-brown

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

InChIKey

LMXYVLFTZRPNRV-XCVCLJGOSA-N

CAS DataBase Reference

220904-83-6

Safety Information

WGK Germany 

3

HS Code 

2933790090

MSDS

• Language:English Provider:SigmaAldrich

GW5074 Usage And Synthesis

Description

GW-5074 (220904-83-6) is a potent inhibitor of cRAF1 kinase (IC50 = 9 nM). Displays 100-fold selectivity for cRAF1 over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm. GW-5074 displays neuroprotective effects in vivo via a mechanism that is independent of MEK, ERK, and Akt signaling. Cell permeable.

Uses

GW5074 has been used as a specific inhibitor of cRaf1 in C2 murine skeletal myoblasts, HT-29 colorectal adenocarcinoma cell line and neutrophils.

Biological Activity

Potent, selective and cell-permeable c-Raf1 kinase inhibitor (IC 50 = 9 nM). Displays ≥ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm.

Biochem/physiol Actions

GW5074 is a cRaf1 kinase inhibitor, which is placed immediately downstream of Ras in the Motogen activated protein kinase (MAPK) signaling pathway. It elicits protection in GW5074 prevents degeneration in Huntington′s disease and also have therapeutic potential in treating neurodegenerative disorders. GW5074 in combination with anti-inflammatory drug, dexamethasone, attenuates sidestream smoke-induced airway inflammation.

storage

Desiccate at -20°C

References

1) Chang et al. (2005), Phorbol 12-myristate 13-acetate upregulates cyclooxygenase-2 expression in human pulmonary epithelial cells via Ras, Raf-1, ERK, and NF-kappaB, but not p38 MAPK pathways; Cell Signal., 217 299 2) Huang et al. (2006), Fibroblast growth factor-2 suppresses oridonin-induced L929 apoptosis through extracellular signal-regulated kinase-dependent and phosphatidylinositol 3-kinase-independent pathway; J. Pharmacol. Sci., 102 305 3) Lackey et al. (2000), The discovery of potent cRaf1 kinase inhibitors; Bioorg. Med. Chem. Lett., 10 223 4) Chen et al. (2004), Bradykinin B2 receptor mediates NF-kappaB activation and cyclooxygenase-2 expression via the Ras/Raf-1/ERK pathway in human airway epithelial cells; J. Immunol., 173 5219

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