GW-5074

SKU: orb1300692

Description

GW 5074 is a potent and selective c-Raf inhibitor (IC50=9 nM) with demonstrated utility in studying MAPK/ERK signaling pathways in cellular and animal models of cancer and neurological diseases. It exhibits high specificity, showing no activity against a panel of other kinases including JNK, MEK, and VEGFR2.

Research Area

Neuroscience

Key Properties

• CAS Number: 220904-83-6
• MW: 521.0
• Purity: >98%
• Formula: C₁₅H₈Br₂INO₂
• SMILES: C(=C1C=2C(NC1=O)=CC=C(I)C2)C3=CC(Br)=C(O)C(Br)=C3
• Target: Kinase
• Solubility: Soluble in DMSO (up to 50 mg/ml).

Bioactivity

• Target IC50:
  C-Raf:9 nM
• 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. GW5074 completely abolishes chronic morphine-mediated AC superactivation I in CHO cells stably expressing the humanμ-opioid receptor. GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice.
• In Vitro:
  GW5074 is a potent and specific inhibitor of c-Raf with IC50 of 9 nM while having 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.
• Cell Research:
  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)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

C-Raf, Apoptosis, inhibit, Inhibitor, GW5074, GW-5074, GW 5074, Raf, Raf kinases, Raf1 Kinase Inhibitor I

Compound Identifiers

PubChem CID

5034