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SJB2-043 inhibits USP1. 8 / 9
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"SJB2-043, first synthesized and reported in 2013, has been demonstrated to inhibit USP1 function, exhibiting cytotoxic effects on leukemic cells [17]."
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"We next determined whether SJB2-043 inhibits the DUB activity of native USP1 complexes isolated from human cells (XREF_FIG)."
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"SJB2-043 inhibited native USP1 in cells, and both compounds promoted the degradation of ID1, ID2, and ID3 in leukemic cell lines, leading to cell death that was partially caspase dependent."
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"SJB2-043 blocked the deubiquitinating enzyme activity of USP1 in vitro with an IC50 in the nanomolar range (Mistry et al., 2013)."
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"Additionally, SJB2-043 has been found to impede the maintenance of cancer stem cells and DNA damage repair by modulating USP1 activity [18]."
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"In addition, SJB2-043 inhibited the labeling of USP1 with Ub-VS in a dose dependent manner (XREF_SUPPLEMENTARY)."
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"USP1 inhibitor SJB2-043 inhibits the enzyme activity of native USP1."
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"These results demonstrate that USP1 inhibitor SJB2-043 inactivates native USP1 in primary AML cells and exhibits cytotoxicity."
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