PI-1840 [Proteasome Inhibitor]

Synthetic. Chemical. CAS: 1401223-22-0. Formula: C22H26N4O3. MW: 394.5. Synthetic. Highly potent, selective and rapidly reversible non-covalent proteasome inhibitor. Targets the chymotrypsin-like beta5-subunit of the constitutive 20S proteasome (IC50=27nM), with minimal crossreactivity on the trypsin-like (beta2) and caspase-like/postglutamyl-peptide-hydrolysis-like (beta1) proteolytic activity (IC50= >100µM, for both). Exhibited over 100-fold selectivity for the constitutive 20S proteasome over the immunoproteasome. Anticancer compound. In vitro, induces the accumulation of proteasome substrates p27, Bax, and IkappaB-alpha, inhibits survival pathways and viability and induces apoptosis in intact cancer cells. Shown to inhibit tumor growth in mice of MDA-MB-231 breast tumors.