KT5720

KT5720 is a kinase inhibitor with specificity towards protein kinase A. It is a semi-synthetic derivative of K252a and analog of staurosporine.

== Physiological Effects == === Protein kinase A === KT5720 is an antagonist of protein kinase A. Protein kinase A (PKA) is a group of kinases that are cAMP-dependent that primarily phosphorylate serine or threonine residues in target proteins. PKA is a tetramer consisting of two catalytic subunits and two regulatory subunits, with the later holding the catalytic subunits in an inactive state. The binding of two cAMP molecules to each regulatory subunit causes an allosteric change that detaches the regulatory subunits from the catalytic subunits. This exposes the ATP-binding site of the kinase. KT5720 binds competitively to the ATP-binding site of the catalytic subunit of PKA and its effects are dependent on the cellular concentration of ATP.