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USP5-IN-1 is an inhibitor of ubiquitin-specific protease 5 (USP5).1 It selectively binds to the zinc finger ubiquitin-binding domain of USP5 (Kd = 2.8 µM) over histone deacetylase 6 (HDAC6), USP3, and USP16 (Kds = >100, 100, and >100 µM, respectively) and USP13, -33, -39, -49, and -51, and BRCA1-associated protein (BRAP) at 1 mM. USP5-IN-1 inhibits the catalytic activity of USP5 using the synthetic Lys48-linked di-ubiquitin (Ub2K48) substrates DU4802 and DU4803 (IC50s = 26 and 0.8 µM, respectively). It decreases tumor volume and weight in a mouse allograft model when administered in combination with an anti-programmed cell death protein 1 (anti-PD-1) antibody.2
WARNING This product is not for human or veterinary use.
1. Structure-
2. USP5-