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.
USP7-IN-1 is a novel selective and reversible inhibitor of USP7 with IC50 of 33 uM; less or no inhibition on USP5, USP8, Uch-L1, Uch-L3 and Caspase(IC50>200 uM); HCT116 cell viability GI50 is 67 uM.
SJB3-019A is a potent and novel usp1 inhibitor. SJB3-019A (IC50 = 0.0781 uM) was 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells.
NSC 687852 is an inhibitor of ubiquitin-specific-processing protease 14 (USP14) and ubiquitin carboxyl-terminal hydrolase isozyme L5 (UCHL5), two proteasome-associated DUBs.
GNE-6640 is a novel selective USP7 inhibitor, inducing tumor cell death. GNE-6640 enhances cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors.
IU1-47 is a potent and specific USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 inhibits IsoT/USP5 with an IC50 of 20 μM. IU1-47 induces tau elimination in cultured neurons.
FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor (Ki=4.2 ?M). FT827 binds to the USP7 catalytic domain (USP7CD; residues 208-560) with an apparent Kd value of 7.8 ?M.
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity.
