Inhibitor of the H2AK119 deubiquitinase BAP1 (IC50 = 0.092 µg/ml). It is selective for BAP1 over UCHL5, USP5,7,8, TNFAIP3-catalytic domain, USP2-catalytic domain, Otubain-1, and Ataxin3. iBAP-II disrupted the BAP1/ASXL3/BRD4 axis via induction of protein degradation of the ASXL3 scaffold protein in the small cell lung cancer lines NCI-H1963, NCI-H748, and NCI-H1882. It also suppressed expression of the master transcription factor ASCL1 in NCI-H1963 small cell lung cancer cells. iBAP-II significantly delayed disease progression in a small cell lung cancer xenograft mouse model.
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