Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 8 µM, 52 µM, against 5-lipoxygenase, Cyclooxygenase, respectively; 6 µM inhibiting the induction of nitric oxide synthase in activated macrophages

Primary Target5-lipoxygenase

Cell permeable: yes

General description

A cell-permeable and irreversible antitumor and anti-inflammatory agent that acts as an inhibitor of 5-lipoxygenase (IC₅₀ = 8 µM) and cyclooxygenase (IC₅₀ = 52 µM). Confers significant protection against neurotoxic and genotoxic agents. Also inhibits the induction of nitric oxide synthase in activated macrophages (IC₅₀ = 6 µM). Recently shown to inhibit the EGF receptor intrinsic kinase activity in the human epidermoid carcinoma A431 cells in a dose- and time-dependent manner. Also shown to be a p300/CREB-binding protein-specific inhibitor of histone acetyltransferase, inhibiting the acetylation of histones H3 and H4 with an IC₅₀ of ~25 µM. Does not affect p300/CREB binding protein-associated factor (PCAF).

A cell permeable antitumor and anti-inflammatory agent that acts as an inhibitor of 5-lipoxygenase (IC₅₀ = 8 µM) and cyclooxygenase (IC₅₀ = 52 µM). Confers significant protection against neurotoxic and genotoxic agents. Also inhibits the induction of nitric oxide synthase in activated macrophages (IC₅₀ = 6 µM). Recently shown to inhibit the EGF receptor intrinsic kinase activity in the human epidermoid carcinoma A431 cells in a dose- and time-dependent manner. Also shown to be a p300/CREB-binding protein-specific inhibitor of histone acetyltransferase, inhibiting the acetylation of histones H3 and H4 with an r>IC₅₀ of ~25 µM. Does not affect p300/CREB binding protein-associated factor (PCAF).

Legal Information

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

Other Notes

Hung, S., et al. 2008. Mol. Pharmacol.74, 274.Cui, L., et al. 2007. Antimicrob. Agents Chemother.51, 488.Salvioli, S., et al. 2007. eCAM4, 181.Balasubramanyam, K. et al. 2004. J. Biol. Chem.279, 51163.Brouet, I., and Okshima, H. 1995. Biochem. Biophys. Res. Commun. 206, 533.Korutla, L., and Kumar, R. 1994. Biochim. Biophys. Acta1224, 597.Flynn, D.L., et al. 1986. Prostagland. Leuk. Med. 22, 357.

Packaging

100 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)