BR-001
Modify Date: 2024-01-11 16:16:20
BR-001 structure
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Common Name | BR-001 | ||
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| CAS Number | 2356113-28-3 | Molecular Weight | 368.409 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C20H17D2FN4O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of BR-001BR-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. |
| Name | BR-001 |
|---|
| Description | 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. |
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| References | 1. Dong H, et al. Cancer Res. 2019 Nov 1;79(21):5587-5596. |
| Molecular Formula | C20H17D2FN4O2 |
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| Molecular Weight | 368.409 |