MS8572 is a selective OTUB1 covalent ligand. MS8572 covalently modifies the noncatalytic cysteine 23 residue of OTUB1 and does not inhibit OTUB1 deubiquitinase activity. MS8572 can be used for development of deubiquitinase-targeting chimeras for targeted protein stabilization [1].
In Vitro, MS8572 covalently modifies purified wild-type human OTUB1 protein, with a modification efficiency of 78%-84% when incubated at a ligand-to-protein ratio of 250:1 for 1 h, and does not inhibit the deubiquitinase activity of purified human OTUB1 protein[1].
References:
[1]. Song X, et al. Discovery of New OTUB1 Covalent Ligands via Structure-Activity Relationship Studies for Targeted Protein Stabilization. J Med Chem. 2026;69(9):10263-10277.
In Vitro, MS8572 covalently modifies purified wild-type human OTUB1 protein, with a modification efficiency of 78%-84% when incubated at a ligand-to-protein ratio of 250:1 for 1 h, and does not inhibit the deubiquitinase activity of purified human OTUB1 protein[1].
References:
[1]. Song X, et al. Discovery of New OTUB1 Covalent Ligands via Structure-Activity Relationship Studies for Targeted Protein Stabilization. J Med Chem. 2026;69(9):10263-10277.