proteasome substrates

PI-1840(IC50 = 27 nM)is a reversible and selective chymotrypsin-like (CT-L) inhibitor, with little proteasome proteolytic effects on trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).

PROTAC CARM1 degrader-1 (compound 3b) is a highly potent degrader (DC50=8.1 nM) of the co-activator associated arginine methyltransferase (CARM1), facilitating its degradation via the VHL-proteasome pathway. By degrading CARM1, it reduces methylation of substrates, such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, inhibiting breast cancer cell migration [1].

PROTAC CARM1 degrader-2 (compound 3e), with a DC50 value of 8.8 nM, is a VHL- and proteasome-dependent degrader of co-activator associated arginine methyltransferase (CARM1). It promotes the degradation of CARM1 and prevents the methylation of its substrates, including poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, consequently inhibiting breast cancer cell migration [1].