Catalog No.: PC-42948Not For Human Use, Lab Use Only.
PI-1840 is a potent, selective, noncovalent, reversible inhibitor for proteasome chymotrypsin-like (CT-L) activity with IC50 of 27 nM, shows no effect on trypsin-like and peptidylglutamyl peptide hydrolyzing activities (IC50>100 uM).
PI-1840 is a potent, selective, noncovalent, reversible inhibitor for proteasomechymotrypsin-like (CT-L) activity with IC50 of 27 nM, shows no effect on trypsin-like and peptidylglutamyl peptide hydrolyzing activities (IC50>100 uM).
PI-1840 also displays 100-fold more selectivity for the constitutive proteasome over the immunoproteasome.
PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α, inhibits survival pathways and viability, and induces apoptosis in intact cancer cells, also sensitizes human cancer cells to the mdm2/p53 disruptor Nutlin.
PI-1840 suppresses the growth in nude mice of human breast tumor xenografts.
