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.
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.
NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination.
