caprotec - functional isolation of proteins made simple

The Stauro caproKit™ represents an ideal kinase profiling system to improve and support drug discovery projects.


Protein kinases play a key role in the regulation of signaling cascades e.g. for cell proliferation, apotosis, or differentiation. Disruption in the regulation of these inter-connected networks are closely associated with diseases like neuronal disorders, cancer, or inflammatory reactions. As many protein kinases are proto oncoproteins or involved in oncogenic signaling a major component towards cancer treatment is the understanding interplay of different signaling cascades to aid in the development of effective therapies.

Staurosporine is a natural product which was originally isolated from the bacterium Streptomyces staurosporeus (1). The interest in this alkaloid resulted from its anti-fungal and anti-hypertensive properties (2). Staurosporine is a potent inhibitor for a large number of serine/threonine kinases, like protein kinase C (PKC), cAMP- and cGMP-dependent protein kinases and also suppresses several tyrosine kinases, like p60v-src, EGF-, or insulin receptor. It binds to many kinases with a preference to ATP-binding proteins with a high affinity but with little selectivity (3). This lack of selectivity has made staurosporine a valuable tool to understand the time-dependent interplay of the different biochemical and signalling pathways, or the structure and function of cellular proteins.

Staurosporine is attached to the Capture Compound™ scaffold and used as selectivity function for the functional isolation of protein kinases and support future drug discovery approaches.



             Downloads

 

             • Stauro caproKit™ Datasheet 10 Rxn

             • Stauro caproKit™ Datasheet 50 Rxn

             • Stauro caproKit™ Guideline

             • Stauro caproKit™ Application Note



The Stauro caproKit can be used to discover and profile protein kinases from a variety of different sources.

 

 


References:

1) S. Omura, Y. Iwai, A. Nakagawa, J. Awaya, H. Tsuchiya, Y. Takahashi, R. Masuma, (1977) A new alkaloid AM-2282 of Streptomyces origin taonomy, fermentation, isolation and preliminiary characterization; J. Antibiot. (30); 275-282.

2) U.T. Rüegg, G.M. Burgess, (1989) Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases; Trends in Pharmacol Sci. (10); 218-220.

3) M.W. Karaman, S. Herrgard, D.K. Treiber, P. Gallant, C.E. Atteridge, B.T. Campbell, K.W. Chan, et al, (2008) A quantitative analysis of kinase inhibitor selectivity; Nat. Biotechnol. (26); 127-132.