GW5074

Synonym(s):3-(3,5-Dibromo-4-hydroxybenzyliden)-5-iodo-1,3-dihydroindol-2-one;5-Iodo-3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-2-indolinone, GW 5074;Raf1 Kinase Inhibitor I - CAS 220904-83-6 - Calbiochem

CAS NO.：220904-83-6
Empirical Formula: C15H8Br2INO2
Molecular Weight: 520.94
MDL number: MFCD09971042
SAFETY DATA SHEET (SDS)
Update Date: 2024-10-28 16:48:35

What is GW5074?

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.

The Uses of GW5074

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

What are the applications of Application

GW 5074 is an inhibitor of c-Raf-1 kinase and PMA-mediated activation of ERK1/2

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

Properties of GW5074

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.
CAS DataBase Reference	220904-83-6

Safety information for GW5074

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.