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Beschreibung

A cell-permeable flavanoid that displays anti-inflammatory, anti-diabetic and anti-cancer properties. Acts as a non-ATP competitive MEK1 inhibitor (IC50<3 µ,M), and ATP-competitive inhibitors of CKI, CKII, IR, MLCK, PKA and PKC (Ki = 9.0 µ,M, 0.6 µ,M, 2.6 µ,M, 1.7 µ,M, 27.5 µ,M and 12.1 µ,M, respectively) and PI 3-Kalpha and PIM-1 (IC50 = 1.8 µ,M and 0.78 µ,M). Reported to inhibit the activities of phosphodiesterase 1-4 (IC50<40 µ,M) and MMP-2 (IC50<24 µ,M in several colorectal carcinoma cells), and block TNFalpha-mediated NF-kappaB signaling (at 50 µ,M in ECV304 cells) and insulin-stimulated glucose transport (Ki ~ 33.5 µ,M in rat adipocytes). Further, induce apoptosis in HL-60 leukemia cells with an IC50 of 43 µ,M., A cell-permeable flavanoid that displays anti-inflammatory, anti-diabetic and anti-cancer properties. Acts as a non-ATP competitive MEK1 inhibitor (IC50<3 µ,M), and ATP-competitive inhibitors of CKI, CKII, IR, MLCK, PKA and PKC (Ki = 9.0 µ,M, 0.6 µ,M, 2.6 µ,M, 1.7 µ,M, 27.5 µ,M and 12.1 µ,M, respectively) and PI 3-Kalpha and PIM-1 (IC50 = 1.8 µ,M and 0.78 µ,M). Reported to inhibit the activities of phosphodiesterase 1-4 (IC50<40 µ,M) and MMP-2 (IC50<24 µ,M in several colorectal carcinoma cells), and block TNFalpha-mediated NF-kappaB signaling (at 50 µ,M in ECV304 cells) and insulin-stimulated glucose transport (Ki = ~ 33.5 µ,M in rat adipocytes). Further, induce apoptosis in HL-60 leukemia cells with an IC50 of 43 µ,M.