Bisindolylmaleimide I

Bisindolylmaleimide I

Bisindolylmaleimide I (also known as BIM I or GF 109203X) is a potent and selective inhibitor of protein kinase C (PKC). It is commonly used in biological research to study the role of PKC in cell function.

Structure and Properties

Bisindolylmaleimide I is a synthetic compound that consists of two indole rings linked by a maleimide group. The indole rings contribute to the compound's ability to interact with the ATP-binding site of PKC, while the maleimide group forms a covalent bond with a cysteine residue in the enzyme's active site. This interaction results in the inhibition of PKC activity.

The compound is soluble in dimethyl sulfoxide (DMSO) and ethanol, but not in water. It is typically stored as a dry powder at -20°C and reconstituted in DMSO immediately before use.

Mechanism of Action

Bisindolylmaleimide I inhibits PKC by binding to the ATP-binding site of the enzyme, preventing ATP from binding and thus blocking the phosphorylation of substrate proteins. This inhibition is non-competitive with respect to ATP, meaning that the inhibitor binds to a different site on the enzyme than ATP.

The compound is selective for PKC, with little effect on other protein kinases. It inhibits all isoforms of PKC, including the conventional, novel, and atypical isoforms.

Applications in Research

Bisindolylmaleimide I is widely used in biological research to study the role of PKC in various cellular processes, including cell proliferation, differentiation, and apoptosis. It has been used in a variety of experimental systems, including cultured cells, animal models, and human tissues.

Safety and Toxicity

Like all laboratory chemicals, bisindolylmaleimide I should be handled with care. It is harmful if swallowed, inhaled, or absorbed through the skin, and it may cause eye irritation. Appropriate safety measures should be taken when handling this compound.

See Also

• Protein kinase C
• Indole
• Maleimide

References

```