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E1/E2/E3 Enzyme E1/E2/E3 Enzyme

Cat.No.  Name Information
M2969 PYR-41 PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.
M31238 M435-1279  M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.
M14330 TAK-243 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.
M14326 Avadomide Avadomide (CC 122) is an orally effective cereblon modulator. avadomide modulates cereblon E3 ligase activity and induces apoptosis in diffuse large B-cell lymphoma (DLBCL) cells. Avadomide has antitumor and immunomodulatory activities. CC-122 is more potent in degrading IKZF1 and IKZF3 than lenalidomide and has broader and enhanced antiproliferative activity in ABC- and GCB-DLBCL cell lines.
M14325 BI8622 BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM.
M11295 Mezigdomide (CC-92480) Mezigdomide (CC-92480) is a novel protein reducing agent and cereblon E3 ligase modulator (CELMoD). Mezigdomide has a strong affinity with Cereblon and has anti-myeloma activity.
M9828 2-D08 2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation.
M9634 TAK-981 TAK-981 is a first-in-class SUMO-activating enzyme inhibitor with superior immune activation and antitumor activity.
M8419 PRT4165 PRT4165 is a potent inhibitor of PRC1 (polycomb-repressive complex 1)-mediated histone H2A ubiquitylation in vivo and in vitro.
M6791 Heclin Heclin is a hECT E3 ubiquitin ligase inhibitor.
M6750 Ginkgolic Acid Ginkgolic Acid is a inhibits SUMOylation by binding E1.
M4846 CC0651 CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme and inhibited the ubiquitination of p27Kip1 with IC50 value of 1.72 μM.
M2892 NSC697923 NSC697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A.
M30020 EN219  EN219 is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC50 of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination.
M29907 RNF5 inhibitor inh-02  RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC50=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research.
M29592 RB-3  RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f, with a Kd of 2.8 μM.
M29433 WS-383  WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
M29432 WS-383 free base  WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
M29429 DI-1859  DI-1859 is a potent, selective and covalent inhibitor of DCN1. DI-1859 inhibits neddylation of cullin 3 in cells at low nanomolar concentrations. DI-1859 induces a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protects mice from acetaminophen-induced liver damage.
M29426 DI-591  DI-591 is a potent, high-affinity and cell-permeable inhibitor of the DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12 nM and 10.4 nM, respectively and has no appreciable binding to DCN3, DCN4, and DCN5 proteins. DI-591 selectively inhibits neddylation of cullin 3 but has no or minimal effect on neddylation of other cullin family members.

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