K252a

K252a is a potent, cell-permeable, reversible, and ATP-competitive inhibitor of protein kinase C (PKC), protein kinase A (PKA), and protein kinase G (PKG). It is often used in biological research to inhibit these kinases. K252a is derived from the bacterium Nocardiopsis.

Structure and Properties

K252a is a staurosporine analog. It has a molecular weight of 467.5 g/mol and a molecular formula of C₂₇H₂₁N₃O₅. The compound is soluble in DMSO and ethanol, but not in water.

Mechanism of Action

K252a inhibits protein kinases by competing with ATP for the ATP-binding site on the kinase. This prevents the kinase from phosphorylating its substrate, thereby inhibiting the kinase's activity. K252a is a potent inhibitor of PKC, PKA, and PKG, with IC₅₀ values in the nanomolar range.

Uses in Research

K252a is commonly used in biological research to inhibit protein kinases. It has been used to study the role of these kinases in various cellular processes, including cell proliferation, differentiation, and apoptosis. K252a has also been used to investigate the mechanisms of various diseases, such as cancer and neurodegenerative diseases.

Safety and Toxicity

K252a is a potent inhibitor of protein kinases and can have toxic effects on cells at high concentrations. Therefore, it should be handled with care and used at the lowest effective concentration.

See Also

• Protein kinase C
• Protein kinase A
• Protein kinase G
• Staurosporine

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