Potent and selective cell permeable inhibitor of cRAF1 kinase (IC50 = 9 nM) with 100-fold selectivity over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm. A useful tool for assessing the involvement of the Ras/Raf-1/ERK pathway in various signaling pathways. Displays neuroprotective effects in vivo through a MEK-ERK and Akt-independent mechanism.
Product Details
| Alternative Name: | 5-Iodo-3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-2-indolinone |
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| Formula: | C15H8Br2INO2 |
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| MW: | 520.9 |
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| CAS: | 220904-83-6 |
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| Purity: | ≥98% (TLC) |
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| Appearance: | Yellow to orange solid. |
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| Solubility: | Soluble in DMSO (>25 mg/ml). |
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| Shipping: | Ambient |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stock solutions are stable for at least 6 months when stored at -20°C. |
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| Handling: | Protect from light. Keep under inert gas. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Fibroblast growth factor-2 suppresses oridonin-induced L929 apoptosis through extracellular signal-regulated kinase-dependent and phosphatidylinositol 3-kinase-independent pathway: J. Huang, et al.; J. Pharmacol. Sci.
102, 305 (2006),
Abstract;
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: M.S. Chang, et al.; Cell Signal.
17, 299 (2005),
Abstract;
Bradykinin B2 receptor mediates NF-kappaB activation and cyclooxygenase-2 expression via the Ras/Raf-1/ERK pathway in human airway epithelial cells: B.C. Chen, et al.; J. Immunol.
173, 5219 (2004),
Abstract;
The c-Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK-ERK and Akt-independent mechanism: P.C. Chin, et al.; J. Neurochem.
90, 595 (2004),
Abstract;
The discovery of potent cRaf1 kinase inhibitors: K. Lackey, et al.; Bioorg. Med. Chem. Lett.
10, 223 (2000),
Abstract;
