Staurosporine and K252a Compounds

Powerful Protein Kinase Inhibitors

Protein phosphorylation constitutes one of the most important molecular mechanisms by which extracellular signals produce their biological responses in eukaryotic cells. Stimulation of protein kinases is considered to be the most common activation mechanism in signal transduction systems¹. The protein serine/threonine kinase can be classified by the nature of their second messenger activators:

1. Ca²⁺/Calmodulin-dependent kinase (CaMK)
2. cAMP-dependent kinase (PKA)
3. Ca²⁺/Phospholipid-dependent kinase (PKC)
4. cGMP-dependent kinase (PKG)
5. And more…²

Staurosporine and K252a are cytotoxic alkaloids, isolated from the culture of Streptomyces staurospores and Nocardiopsis sp. respectively^3,4. These unique toxins represent a second generation of protein-kinase inhibitors⁵.

We are pleased to make available for research highly pure Staurosporine, K252a and its derivatives, K252b, KT5720 and KT5823. All of these compounds are offered in small convenient and large (econo) sizes at reasonable prices which, we believe should facilitate in vitro and in vivo experiments which were not economically feasible before.

References

1. Walaas, S.I. and Greengard, P. (1991) Pharmacol. Rev. 43, 299.
2. Nairn, A.C. et al. (1985) Ann.Rev.Biochem. 54, 931.
3. Omura, S. et al. (1995) J. Antibiotics 48, 535.
4. Nakanishi, S. et al. (1986) J. Antibiotics 39, 1066.
5. Matsuda, Y. (1993) Actinomycetology 7, 110.