Chloromethylketone-EGR, (EGRCK) FITC

Tri-peptide chloromethylketones have been utilized extensively to irreversibly inhibit various serine proteases (1-5). Among the most common chloromethylketones are FPRCK (Phe-Pro-Arg-chloromethylketone), which is a rapid inhibitor of a-thrombin and EGRCK (Glu-Gly-Arg-chloromethylketone), which rapidly inhibits factor Xa (1). Recently, the modification of these tri-peptide chloromethylketones with reporting groups, such as fluorescent probes (6-8), radioactive labels (9) or thioreactive-labels (10), has provided a unique approach to the study of various serine proteases. These probes are useful because they allow a means of reporting molecular changes in an enzyme, and not its zymogen, while also inhibiting the enzymatic activity. \n\nApplications: The fluorescein labeled compounds are useful in both Western blot and fluorescent imaging applications.\n\nStorage and Stability: May be stored at 4 degrees C for short-term only. For long-term storage, store at -20 degrees C. Aliquots are stable for at least 6 months at -20 degrees C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.\n\nAdditional Specifications:\nSpecial Properties: Tri-peptide chloromethyl ketones are very potent and irreversible inhibitors of serine proteases. BFPRCK is especially useful for inhibition of thrombin and tPA, while BEGRCK is useful for inhibition of factor Xa.

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SPECIFICATIONS

Catalog Number

C5026

Size

1mg

Applications

IF, WB

Form

Supplied as a liquid in 10mM HCl.

Purity

Fluorescein labelled EGRCK is prepared by the method of Williams et al. (11).

References

1. Kettner, C. and Shaw, E., Methods Enzymol., 80, 826 (1981).\n2. Ganu, V.S. and Shaw, E., Thromb. Res., 45, 1 (1987).\n3. Kettner, C. and Shaw, E., Biochim. Biophys. Acta, 569, 31 (1979).\n4. Kettner, C., et al., Arch. Biochem. Biophys., 202, 420 (1980).\n5. Kettner, C. and Shaw, E., Bochemistry, 17, 4778 (1978).\n6. Kettner, C. and Shaw, E., Thromb. Res., 22, 645 (1981).\n7. Lollar, P. and Fass, D.H., Arch. Biochem. Biophys., 233, 438 (1984).\n8. Boskovic, D.S., et al., J. Biol. Chem., 265, 10497 (1990).\n9. Rauber, P., et al., Anal. Biochem., 168, 259 (1988).\n10. Bock, P.E., Biochemistry, 27, 6633 (1988).\n11. Williams, E.B., et al., J. Biol. Chem., 264, 7536, (1989).\n12. Mann, K.G., et al., Blood, 76, 755 (1990).\n13. Hartshorn, J.N., et al., Blood, 78, 833 (1991).