WP1130 (Degrasyn) is a novel selective small molecular deubiquitinase inhibitor and a Bcr/Abl destruction pathway activator that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells.
NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45??4 μM, 37??1 μM, and 9.8??1.8 μM, respectively.
NSC 687852 is an inhibitor of ubiquitin-specific-processing protease 14 (USP14) and ubiquitin carboxyl-terminal hydrolase isozyme L5 (UCHL5), two proteasome-associated DUBs.
CB-5083 is a novel first in class, potent orally bio-available p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models .
N106, activator of SUMO-activating enzyme, E1 ligase. Increases SERCA2a SUMOylation and activity, and enhances contractility in rat cardiomyocytes in vitro.
2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.
Avadomide(CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4CRBN.
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity.
