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

Inhibitors

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.
M14331 TZ9 TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.
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.
M14329 SMIP004 SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells.
M14328 NSC232003 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.
M14327 DKM 2-93 DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
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.
M10899 VII-31 VII-31 is a NEDDylation pathway activator that suppresses tumors in vivo and in vitro. VII-31 also induces apoptosis.
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.
M6750 Ginkgolic Acid Ginkgolic Acid is a inhibits SUMOylation by binding E1.
M2969 PYR-41 PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.



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