11-anilino-7,8,9,10-tetrahydrobenzimidazo[1,2-b]isoquinoline-6-carbonitrile

Biological Activity

Cell-permeable and potent inhibitor of ubiquitin specific peptidase 22 (USP22) th at exhibits anticancer activity.


Usp22i-S02 is a cell-permeable benzimidazoisoquinoline-carbonitrile analog th at is shown to reversibly occupy USP22 (ubiquitin specific peptidase 22) catalytic domain and suppress its functions. Usp22i-S02 arrests Usp22-mediated Foxp3 deubiquitination in iTREG cells in a time and dose-dependent manner. Usp22i-S02 administration enhances antitumor immunity with low toxicity in LLC1-challenged mice (20 mg/kg) and reduces tumor burden in a Treg-specific manner. immunity with low toxicity in LLC1-challenged mice (20 mg/kg) and reduces tumor burden in a Treg-specific manner.