Ubiquitin (UB) is a protein modifier that regulates many essential cellular processes. To initiate protein modification by UB, the E1 enzyme activates the C-terminal carboxylate of UB to launch its transfer through the E1-E2-E3 cascade onto target proteins. The E1 enzyme is the activating enzyme, to which ubiquitin is attached in an ATP-dependent reaction by a thioester bond. The E2 enzyme is the conjugating enzyme, to which the ubiquitin is transferred from the E1. The E3 is the ubiquitin ligase, which directly or indirectly catalyzes the transfer of the ubiquitin to the target protein (the substrate), with the formation of an isopeptide bond.
||PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation.
||TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.
||CC-122 is a novel agent for DLBCL with antitumor and immunomodulatory activity.
||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.
||SZL P1-41 is Skp2 inhibitor, selectively suppresses Skp2 E3 ligase activity, but not activity of other SCF complexes.
||Ginkgolic Acid is a natural compound with suspected cytotoxic, allergenic, mutagenic and carcinogenic properties, and it can inhibit protein SUMOylation both in vitro and in vivo without affecting in vivo ubiquitination.
||PYZD-4409 is a novel small molecule inhibitor of Ubiquitin-activating enzyme UBA1/E1 enzyme with an IC50 of 20 uM (cell-free enzymatic assay).
||Skp2 Inhibitor C1
||Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.
||DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
||DI-591 (DI591) is a potent, selective, cell-permeable inhibitor of the DCN1-UBC12 interaction with Ki of 10-12 nM for human DCN1 and DCN2.
||DI-404 is a highly potent, peptidomimetic inhibitor of DCN1-UBC12 protein-protein interaction that bind to DCN1 protein with Kd of 6.9 nM, selectively inhibits the neddylation of cullin 3 over other cullin members.
||NAcM-COV is a specific, irreversible small molecule inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 with IC50 of 28 nM in TR-FRET assays.
||NAcM-OPT is a specific, reversible small molecule inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 with IC50 of 79 nM in TR-FRET assays.
||GSK145A is a small molecule inhibitor of SUMO-conjugating enzyme E2 with IC50 of 12.5 uM, GSK145A is competitive with the sumoylation of the TRPS1 peptide substrates.
||TAK-243 (MLN-7243, AOB87172) is a small-molecule, cell-permeable inhibitor of ubiquitin-activating enzyme E1 (UAE1).
||A nonselective inhibitor of UBL protein-activating E1 enzymes that forms covalent adducts with UBL proteins SUMO1, ubiquitin, Nedd8, ISG15, and GABARAP in the presence of ATP and E1 enzymes in vitro
||A potent, covalent inhibitor of ubiquitin-conjugating enzyme UbcH5 with Kd of 5.189 uM, 3.578 uM, and 2.577 uM for UbcH5a, UbcH5b, and UbcH5c, respectively
||ABP-A3(ABP A3) is an inhibitor of ubiquitin conjugation that targets ubiquitin and Nedd8 E1 enzymes