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Chemical Structure : BR-001
Catalog No.: PC-73067Not For Human Use, Lab Use Only.
BR-001 (BR001) is a potent, selective, allosteric inhibitor of EED subunit of PRC2 complex, disrupts EED-H3K27me3 interaction (IC50=4.5 nM).
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BR-001 (BR001) is a potent, selective, allosteric inhibitor of EED subunit of PRC2 complex, disrupts EED-H3K27me3 interaction (IC50=4.5 nM).
BR-001 directly binds to EED in the H3K27me3-binding pocket, BR-001 significantly increases the thermal stability of EED in thermal shift assay.
BR-001 is selective for EED, has no activity against 371 wild-type kinases.
BR-001 significantly reduced the cellular H3K27me3 level and also exhibited a strong antiproliferative effect in Karpas 422 cells.
BR-001 inhibited proliferation of DLBCL cells and tumor growth, and upregulated target genes expression.
BR-001 has potent antitumor efficacy in vivo, modulates immune response to suppress syngeneic CT26 colon tumor.
| M.Wt | 368.409 | |
| Formula | C20H17D2FN4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Dong H, et al. Cancer Res. 2019 Nov 1;79(21):5587-5596.
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