Biochem/physiol Actions

Reversible: no

Target K_i: 120 nM, 230 nM, 100 nM, and 600 pM, against calpain I, calpain II, cathepsin B, and cathepsin L, respectively

Product does not compete with ATP.

Primary Targetcalpain-1

Cell permeable: yes

General description

A cell-permeable inhibitor of calpain I (K_i = 120 nM), calpain II (K_i = 230 nM), cathepsin B (K_i = 100 nM), and cathepsin L (K_i = 0.6 nM). Inhibits activation-induced programmed cell death and restores defective immune responses in HIV⁺ donors. Also prevents nitric oxide produced by activated macrophages by interfering with transcription of the inducible nitric oxide synthase gene.

Cell permeable inhibitor of calpain I (K_i = 120 nM), calpain II (K_i = 230 nM), cathepsin B (K_i = 100 nM), and cathepsin L (K_i = 600 pM). Inhibits activation-induced programmed cell death and restores defective immune responses in HIV⁺ donors. Blocks nitric oxide production by activated macrophages by interfering with transcription of the inducible nitric oxide synthase gene. A weak inhibitor of proteasome.

Legal Information

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

Other Notes

Ravid, T., et al. 2000. J. Biol. Chem.275, 35840.Griscavage, J.M., et al. 1995. Biochem. Biophys. Res. Commun.215, 721.Sarin, A., et al. 1994. J. Immunol.153, 862.Sarin, A., et al. 1993. J. Exp. Med. 178, 1693.Banik, N.L., et al. 1992. Neurochem. Res.17, 797.Koohmaraie, M. 1992. Biochemie74, 239.Pinter, M., et al. 1992. Biochemistry31, 8201.Shenoy, A.M., and Brahmi, Z. 1991. Cell. Immunol.138, 24.Sasaki, T., et al. 1990. J. Enzyme Inhib.3, 195.

Packaging

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.

Sequence

N-Acetyl-Leu-Leu-Met

Warning

Toxicity: Standard Handling (A)