General description
A cell-permeable, irreversible inhibitor of cysteine proteases. Similar to E-64 (Cat. No. 324890) but devoid of charged groups. Reported to inhibit calpain-1 activation. The inhibitory activity of EST has been attributed to E-64c, the free acid formed by hydrolysis of the ester in vivo. Used in animal models of muscular dystrophy.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
calpain-1
Product does not compete with ATP.
Reversible: no
Target IC50: 10-100 µM for calpain-1
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for 6 months at -20°C.
Other Notes
Inomata, M., et al. 1996. Arch. Biochem. Biophys. 328, 129.
Mehdi, S. 1991. Trends Biochem. Sci. 16, 150.
McGowan, E.B., et al. 1989. Biochem. Biophys. Res. Commun.158, 432.
Tamai, M., et al. 1987. J. Pharmacobiodyn.10, 678.
Komatsu, K., et al. 1986. Exp. Neurol. 91, 23.
Tamai, M., et al. 1986. J. Pharmacobiodyn. 9, 672.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
| Quality Level | 100 |
| description | RTECS - RR0404300 |
| assay | ≥97% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze |
| color | white |
| solubility | DMSO: soluble |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | N([C@@H](CC(C)C)C(=O)NCCC(C)C)C(=O)[C@H]1O[C@@H]1C(=O)OCC |
| InChI | 1S/C17H30N2O5/c1-6-23-17(22)14-13(24-14)16(21)19-12(9-11(4)5)15(20)18-8-7-10(2)3/h10-14H,6-9H2,1-5H3,(H,18,20)(H,19,21)/t12-,13-,14-/m0/s1 |
| InChI key | SRVFFFJZQVENJC-IHRRRGAJSA-N |
