The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNF-α-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.1
1
Heynekamp, J.J., Weber, W.M., Hunsaker, L.A., et al. Subsitituted trans-stilbenes, including analogues of the natural product resveratrol, inhibit the human tumor necrosis factor α-induced activation of transcription factor nuclear factor κB. J Med Chem497182-7189(2006).
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COc1ccc(cc1)\C=C/c1ccccc1F
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Heynekamp, J.J., Weber, W.M., Hunsaker, L.A., et al. Subsitituted trans-stilbenes, including analogues of the natural product resveratrol, inhibit the human tumor necrosis factor α-induced activation of transcription factor nuclear factor κB. J Med Chem497182-7189(2006).
CAY10512 is available in the following screening
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