| S7165 |
UNC1999
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UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. This compound is a potent autophagy inducer. It specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis.
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Cell Stem Cell, 2025, S1934-5909(25)00041-4
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Cell Rep, 2025, 44(5):115673
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bioRxiv, 2025, 2025.05.22.655558
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| S7656 |
CPI-360
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CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
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Nature Communications, 2024, 4770
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Protein & Cell, 2022, 683-688
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Mol Ther Oncolytics, 2022, 27:14-25
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