Immunoproteasome inhibitor 1

Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (Kis of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the treatment of certain neoplastic diseases[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome

β5c submit:1.18 μM (Ki)

β1i submit:0.27 μM (Ki)

β2i submit:20 μM (Ki)

β5i submit:1.91 μM (Ki)

Immunoproteasome inhibitor 1 (compound 9) (0-25 μM; 0-600 seconds; in Human 20S immunoproteasome and human 20S proteasome) has high binding affinity for the β1i subunit (0.27 µM) of immunoproteasome and proteasome, coupling with good inhibitory properties towards β5i and β5c subunits. And the results of against the β5i subunit shows that the inhibition is reversible, time-independent[1].

[1]. Ettari R, et al. Development of isoquinolinone derivatives as immunoproteasome inhibitors. Bioorg Med Chem Lett. 2022;55:128478.