E1 activating

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  1. Ubiquitin E1 Inhibitor

    PYR-41 is a cell-permeable, irreversible ubiquitin-activating enzyme (E1) inhibitor (IC50 < 10 μM).
  2. SUMO-activating enzyme activator

    N106, activator of SUMO-activating enzyme, E1 ligase. Increases SERCA2a SUMOylation and activity, and enhances contractility in rat cardiomyocytes in vitro.
  3. SAE inhibitor

    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.
  4. SUMO inhibitor

    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.
  5. SUMO E1 Inhibitor

    COH000 is a highly specific covalent allosteric SUMO E1 inhibitor with an IC50 of 0.2 μM for SUMOylation in vitro.
  6. UWE1 ubiquitin ligase inhibitor

    BI-8622 is a specific inhibitor of the HUWE1 ubiquitin ligase.
  7. HUWE1 inhibitor

    BI-8626 is a specific inhibitor of the HUWE1 ubiquitin ligase with an IC50 of 0.9 μM.
  8. 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.
  9. SUMO inhibitor

    TAK-981 is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.
  10. UBA5 inhibitor

    DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
  11. UAE (UBA1) inhibitor

    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.
  12. UBA1 inhibitor

    PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay).

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