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).

PROTACEZH2 Degrader-9 is an orally active EZH2 PROTAC degrader, operating through the ubiquitin-proteasome pathway. It effectively reduces the PRC2 core subunit and potently inhibits H3K27me3 without affecting common CRBN neo-substrates, showing selectivity towards GSPT1 and IKZF1/3. The compound exhibits strong antiproliferative effects on various cancer cell lines by inducing cell cycle arrest and apoptosis (apoptosis). Additionally, PROTACEZH2 Degrader-9 reverses PRC2-mediated gene silencing and suppresses the activation of EZH2 non-catalytic target genes. This compound is applicable in research on leukemia, lymphoma, and non-small cell lung cancer.

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].

Anti-Polyubiquitin Antibody represents a highly specialized monoclonal antibody specifically engineered to target the complex lysine-linked polyubiquitin chains with exceptional binding affinity and selectivity, effectively facilitating the measurable detection and quantification of polyubiquitinated substrates across various preclinical experimental models to evaluate the dynamic regulation of the ubiquitin-proteasome system during strictly monitored laboratory observation periods.