General description

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

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Lee, K.W., et al. 2007. Carcinogenesis28, 1918.Holder, S., et al. 2007. Mol. Cancer Ther.6, 163.Strobel, P., et al. 2005. Biochem. J.386, 471.Ko, C.H., et al. 2005. Mol. Cancer Ther.4, 281.Ko, C.H., et al. 2005. Biochem. Pharmacol.69, 913.Ko, W.C., et al. 2004. Biochem. Pharmacol.68, 2087.Walker, E.H., et al. 2000. Mol. Cell6, 909.Agullo, G., et al. 1997. Biochem. Pharmacol.53, 1649.Hagiwara, M., et al. 1988. Biochem. Pharmacol.37, 2987.

Packaging

Packaged under inert gas

25 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)