ML-792 | SUMO-activating enzyme inhibitor

ML-792 Supplier | CAS 1644342-14-2 | Focus Biomolecules

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ML-792 (1644342-14-2) is a potent (IC50’s = 3 nM SUMO1; 11 nM SUMO2) and selective ( IC50 = 32 µM for NEDD8-activating enzyme (NAE)) mechanism-based inhibitor of SUMO-activating enzyme (SAE).1 Treatment of multiple cancer cell lines led to failure of mitotic progression and induction of endoreduplication with MYC-amplified cell lines showing higher sensitivity.  ML-792 inhibited B-cell growth and promoted cell death in Epstein-Barr virus (EBV)-positive B cells and nasopharyngeal carcinoma cells.  It also modulated Latent Membrane Protein-1-induced cell migration and cell adhesion suggesting therapeutic potential in treating EBV-associated malignancies.2

References/Citations:

  1. He et al. (2017), Probing the roles of SUMOylation in cancer cell biology by using a selective SAE inhibitor; Nat. Chem. Biol. 13 1164
  2. Garcia et al. (2021); Effects of targeting sumoylation processes during latent and induced Epstein-Barr virus infections using the small molecules inhibitor ML-792, Antiviral Res., 188 105038
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Alternate Name:
VU0485891

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ML-792 (1644342-14-2) is a potent (IC50’s = 3 nM SUMO1; 11 nM SUMO2) and selective ( IC50 = 32 µM for NEDD8-activating enzyme (NAE)) mechanism-based inhibitor of SUMO-activating enzyme (SAE).1 Treatment of multiple cancer cell lines led to failure of mitotic progression and induction of endoreduplication with MYC-amplified cell lines showing higher sensitivity.  ML-792 inhibited B-cell growth and promoted cell death in Epstein-Barr virus (EBV)-positive B cells and nasopharyngeal carcinoma cells.  It also modulated Latent Membrane Protein-1-induced cell migration and cell adhesion suggesting therapeutic potential in treating EBV-associated malignancies.2

References/Citations:

  1. He et al. (2017), Probing the roles of SUMOylation in cancer cell biology by using a selective SAE inhibitor; Nat. Chem. Biol. 13 1164
  2. Garcia et al. (2021); Effects of targeting sumoylation processes during latent and induced Epstein-Barr virus infections using the small molecules inhibitor ML-792, Antiviral Res., 188 105038