GW-5074 | c-Raf1 inhibitor

CAS:
220904-83-6
Catalog Number:
10-1031
Activity:
c-Raf1 inhibitor
Chemical Name:
3-(3,5-Dibromo-4-hydroxybenzylidene)-5-iodo-1,3-dihydroindol-2-one
Molecular Weight:
520.95
Molecular Formula:
C15H8Br2INO2
Solubility:
Soluble in DMSO (up to 50 mg/ml).
Physical Properties:
Dark orange solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$60.00
25 mg$185.00

GW-5074 (220904-83-6) is a potent inhibitor of cRAF1 kinase (IC50 = 9 nM).1 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. GW-5074 was able to reduce mutant huntingtin protein (mHTT) levels but not wild-type via linking mHTT to LC3 leading to autophagic degradation.5 A promising new strategy in the field of targeted protein degradation via utilization of autophagy. Cell permeable.

References/Citations:

1) Lackey et al. (2000), The discovery of potent cRaf1 kinase inhibitors; Bioorg. Med. Chem. Lett., 10 223
2) 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
3) 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
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
5) Li et al. (2019), Allele-selective lowering of mutant HTT protein by HTT-LC3 linker compounds; Nature, 575 203

CAS:
220904-83-6
Catalog Number:
10-1031
Activity:
c-Raf1 inhibitor
Chemical Name:
3-(3,5-Dibromo-4-hydroxybenzylidene)-5-iodo-1,3-dihydroindol-2-one
Molecular Weight:
520.95
Molecular Formula:
C15H8Br2INO2
Solubility:
Soluble in DMSO (up to 50 mg/ml).
Physical Properties:
Dark orange solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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