K252a is an

alkaloid Alkaloids are a class of basic, naturally occurring organic compounds that contain at least one nitrogen atom. This group also includes some related compounds with neutral and even weakly acidic properties. Some synthetic compounds of simila ...

isolated from '' Nocardiopsis''

bacteria Bacteria (; singular: bacterium) are ubiquitous, mostly free-living organisms often consisting of one biological cell. They constitute a large domain of prokaryotic microorganisms. Typically a few micrometres in length, bacteria were am ...

. This staurosporine analog is a highly potent cell permeable

inhibitor Inhibitor or inhibition may refer to: In biology * Enzyme inhibitor, a substance that binds to an enzyme and decreases the enzyme's activity * Reuptake inhibitor, a substance that increases neurotransmission by blocking the reuptake of a neurotra ...

of CaM

kinase In biochemistry, a kinase () is an enzyme that catalyzes the transfer of phosphate groups from high-energy, phosphate-donating molecules to specific substrates. This process is known as phosphorylation, where the high-energy ATP molecule don ...

and phosphorylase kinase (IC₅₀ = 1.8 and 1.7 nmol/ L, respectively). At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC₅₀ of 10 to 30 nmol/L).Tapley, P. ''et al.'' (1992) Oncogene 7, 371. K252a is reported to promote myogenic differentiation in C2 mouse myoblasts and has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase activity. K252a has been reported in preclinical research as a potential treatment for

psoriasis Psoriasis is a long-lasting, noncontagious autoimmune disease characterized by raised areas of abnormal skin. These areas are red, pink, or purple, dry, itchy, and scaly. Psoriasis varies in severity from small, localized patches to comple ...

Promising New Treatments for Psoriasis,

Sarah Dubois Declercq and Roxane Pouliot >.

The Scientific World Journal; Volume 2013, Article ID 980419; https://dx.doi.org/10.1155/2013/980419

K252a inhibits tyrosine

phosphorylation In chemistry, phosphorylation is the attachment of a phosphate group to a molecule or an ion. This process and its inverse, dephosphorylation, are common in biology and could be driven by natural selection. Text was copied from this source, wh ...

of Trk A induced by NGF. PC12 cells were incubated in the presence or absence of 10 ng/ml NGF with or without various concentrations of K252a.

See also

References

Further reading