Street Address: 45-1 Ramsey Road, Shirley, Ny 11967, Usa
Country/Region: United States
Inhibition
Equivalent to the IC50 for wild-type PI3K-alpha, PKI-402 inhibits E545K and H1047R PI3K-alpha mutants with IC50 of 3 nM. Enzyme inhibitors are molecules that interact in certain ways with the enzyme to prevent it from functioning in a normal manner. They can alter the catalytic action of the enzyme and consequently slow down, or even stop catalysis. Inhibitors can act in various modes when interacting with the enzyme: reversible or irreversible inhibition, covalent binding or non-covalent binding, as well as specific or nonspecific inhibition. Based on the inhibition kinetics, enzyme inhibition can be categorized into three major types: competitive inhibition, non-competitive inhibition, and uncompetitive inhibition.