General description
A cell-permeable inhibitor of calpain I (Ki = 120 nM), calpain II (Ki = 230 nM), cathepsin B (Ki = 100 nM), and cathepsin L (Ki = 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 (Ki = 120 nM), calpain II (Ki = 230 nM), cathepsin B (Ki = 100 nM), and cathepsin L (Ki = 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
calpain-1
Product does not compete with ATP.
Reversible: no
Target Ki: 120 nM, 230 nM, 100 nM, and 600 pM, against calpain I, calpain II, cathepsin B, and cathepsin L, respectively
Warning
Toxicity: Standard Handling (A)
Sequence
N-Acetyl-Leu-Leu-Met
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 41181721
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 208721-25MG
