ML-792

ML-792 is an inhibitor of SUMO-activating enzyme (SAE; IC₅₀s = 0.003 and 0.011 µM with small ubiquitin-related modifier 1 (SUMO-1) or SUMO-2, respectively, as the ubiquitin-like proteins).¹ It is selective for SAE over NEDD8-activating enzyme (NAE) and ubiquitin-activating enzyme (UAE; IC₅₀s = 32 and >100 µM, respectively). ML-792 inhibits SAE activity and decreases global SUMOylation in HCT116 human colon cancer cells (EC₅₀ = 0.019 µM), as well as decreases the viability of MDA-MB-468 human breast and A375 human melanoma cells (EC₅₀s = 0.06 and 0.45 µM, respectively). It also induces mitotic defects in HCT116 cells and impairs chromosomal segregation in HCT116, A375, and COLO 205 cells. ML-792 reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 150 and 200 mg/kg twice per day.²

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1. He, X., Riceberg, J., Soucy, T., et al. Probing the roles of SUMOylation in cancer cell biology by using a selective SAE inhibitor. Nat. Chem. Biol. 13(11), 1164-1171 (2017).

2. Langston, S.P., Grossman, S., England, D., et al. Discovery of TAK-981, a first-in-class inhibitor of SUMO-activating enzyme for the treatment of cancer. J. Med. Chem. 64(5), 2501-2520 (2021).