N^α-Tosyl-Lys Chloromethyl Ketone, Hydrochloride

Inhibits trypsin-like serine proteases. Inactivates trypsin irreversibly without affecting chymotrypsin. Prevents nitric oxide production by activated macrophages by interfering with transcription of the iNOS gene. Blocks cell-cell adhesion and binding of HIV-1 virus to target cells. In macrophages, blocks nitric oxide synthase induced by interferon-γ and lipopolysaccharides (EC₅₀ = 80 µM). Prevents endonucleolysis accompanying apoptotic death of HL-60 leukemic cells and normal thymocytes. Suggesting working concentration is 10-100 µM.

Inhibits trypsin-like serine proteinases. Irreversibly inactivates trypsin without affecting chymotrypsin. Prevents nitric oxide production by activated macrophages by interfering with transcription of the iNOS gene. Blocks cell-cell adhesion and binding of HIV-1 virus to the target cells. In macrophages, blocks nitric oxide synthase induced by interferon-γ and lipopolysaccharides (EC₅₀ = 80 µM). Prevents endonucleolysis accompanying apoptotic death of HL-60 leukemia cells and normal thymocytes.

Cell permeable: no

EC50 = 80 µM blocking nitric oxide synthase induced by interferon-γ and lipopolysaccharides in macrophages

Primary Target
trypsin like proteases

Product does not compete with ATP.

Reversible: no

Unstable in solution; reconstitute just prior to use.

Griscavage, J.M., et al. 1995. Biochem. Biophys. Res. Commun.215, 721.
Kim, H., et al. 1995. J. Immunol.154, 4741.
Bourinbaiar, A.S. and Nagorny, R. 1994. Cell Immunol. 155, 230.
Biro, A., et al. 1992. Eur. J. Immunol.22, 2547.
Bruno, S., et al. 1992. Leukemia6, 1113.
Lee, S.F. 1992. Infect. Immun. 60, 4032.
Schmidt, H.H., et al. 1992. Mol. Pharmacol.41, 615.

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

Toxicity: Irritant (B)