Chemical Structure : UNC4976
货号: PC-38261Not For Human Use, Lab Use Only.
UNC4976 (UNC-4976) is a potent cellular active positive allosteric modulator of CBX7, binds to CBX7 competitively with H3K27me3 peptides (IC50=20 nM), while increasing affinity for oligonucleotides.
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UNC4976 (UNC-4976) is a potent cellular active positive allosteric modulator of CBX7, binds to CBX7 competitively with H3K27me3 peptides (IC50=20 nM), while increasing affinity for oligonucleotides.
UNC4976 displays >40-fold selectivity over CBX8 (IC50=890 nM).
The PAM activity of UNC4976 resulted in enhanced efficacy across three orthogonal cellular assays by simultaneously antagonizing H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
UNC4976 reequilibrates PRC1 away from H3K27me3 target regions.
分子量 | 847.111 | |
分子式 | C47H70N6O8 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Kelsey N Lamb, et al. Cell Chem Biol. 2019 Oct 17;26(10):1365-1379.e22.
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