General description
Calpeptin inhibits the Ca2+-stimulatedcleavage of p35 to p25 by calpain. It regulates the processing of β-amyloidprecursor protein to β-amyloid (Aβ). Calpeptin alleviates neurite elongation indifferentiating PC12 cells. In platelets, it prevents Ca2+-ionophore-induceddegradation of actin binding protein and P235. It blocks the myosinlight chain phosphorylation in platelets stimulated by collagen, ionomycin, orthrombin. Calpeptin inhibits the growth of estrogen receptor positive breast cancer cells. Calpeptin is a cell permeable calpain blocker. It also blocks theactivation of T-cells in the immune system. It has been observed that calpeptininduces secondary inflammatory responses and apoptosis in muscle cells.
Biochem/physiol Actions
Cell permeable: yes
ID50 = 52 nM for calpain-1; 34 nM for calpain-2; 138 nM for papain
Product does not compete with ATP.
Reversible: no
Packaging
Packaged under inert gas
Preparation Note
Dissolve in a minimal amount of DMF or DMSO then add H₂O, buffer or medium just prior to use.
Other Notes
Lee, M.S., et al. 2000. Nature405, 360.
Yamazaki, T., et al. 1997. Biochemistry27, 8377.
Klafki, H., et al. 1996. J. Biol. Chem.271, 28655.
Shiba, E., et al. 1996. Anticancer Res. 16, 773.
Pinter, M., et al. 1994. Neurosci. Lett. 170, 91.
Saito, K., and Nixon, R.A. 1993. Neurochem. Res. 18, 231.
Tsujinaka, T., et al. 1988. Biochem. Biophys. Res. Commun.153, 1201.
Z-Leu-Nle-CHO
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥94% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze |
| color | white to off-white |
| solubility | DMF: 5 mg/mL,DMSO: 5 mg/mL |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | N([C@@H](CC(C)C)C(=O)N[C@@H](CCCC)C=O)C(=O)OCc1ccccc1 |
| InChI | 1S/C20H30N2O4/c1-4-5-11-17(13-23)21-19(24)18(12-15(2)3)22-20(25)26-14-16-9-7-6-8-10-16/h6-10,13,15,17-18H,4-5,11-12,14H2,1-3H3,(H,21,24)(H,22,25)/t17-,18-/m0/s1 |
| InChI key | PGGUOGKHUUUWAF-ROUUACIJSA-N |
