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Chemical Structure : DC-PRC2in-01
Catalog No.: PC-20124Not For Human Use, Lab Use Only.
DC-PRC2in-01 is a small molecule PRC2 inhibitor targeting EZH2-EED interaction with affinity Kd of 4.56 uM, decreases global H3K27me3 levels in cancer cells.
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DC-PRC2in-01 is a small molecule PRC2 inhibitor targeting EZH2-EED interaction with affinity Kd of 4.56 uM, decreases global H3K27me3 levels in cancer cells.
DC-PRC2in-01 shows an IC50 of 4.21 μM for bindingt to EED in the fluorescence polarization (FP) competitive binding assays.
DC-PRC2in-01 destabilizes the PRC2 complex, thereby leading to the degradation of PRC2 core proteins and the decrease of global H3K27me3 levels in cancer cells.
DC-PRC2in-01 effectively inhibits the proliferation of PRC2-driven lymphomas cells, arrested the cell cycle in the G0/G1 phase.
DC-PRC2in-01 shows growth inhibition effects on cancer cells, including Pfeiffer, KARPAS422, SU-DHL-4, and DB, via a cell viability assay (IC50s=3.5-10 uM).
| M.Wt | 444.55 | |
| Formula | C27H29FN4O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Daohai Du, et al. J Med Chem. 2021 Jun 24;64(12):8194-8207.
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