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.
SMER3 is a selective inhibitor of a yeast SCF family E3 ubiquitin ligase (SCFMet30) in vitro and in vivo. Induces the expression of MET genes; blocks cell proliferation.
HLI 373 is an inhibitor of Hdm2 ubiquitin ligase (E3) which blocks Hdm2-mediated ubiquitylation, proteasomal degradation of p53 and activates p53-dependent transcription.
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.
ML-792 is a potent and selective SAE inhibitor with nanomolar potency in cellular assays. ML-792 selectively blocks SAE enzyme activity and total SUMOylation, thus decreasing cancer cell proliferation.
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.
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.
MSC1094308 is a reversible and allosteric inhibitor of the type II AAA ATPase human ubiquitin-directed unfoldase (VCP)/p97 and the type I AAA ATPase VPS4B, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively.
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.
Teslexivir (BTA074; AP 611074) is a topical antiviral agent that is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an interaction that is a necessary step for Human Papilloma Virus (HPV) 6 and 11 DNA replication and thus viral production.
