PFI 4 |
| カタログ番号GC10979 |
PFI 4 (化合物 11) は、強力で選択性の高い BRPF1 ブロモドメイン (BRPF1B) 阻害剤であり、IC50 は 172 nM です。 PFI 4 は、HBO1/BRPF1 複合体の機能メカニズムを調査し、骨損失および溶骨性悪性骨病変を研究するために使用できます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 900305-37-5
Sample solution is provided at 25 µL, 10mM.
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PFI 4 is a cell permeable, potent and selective inhibitor of BRPF1 Bromodomain with pIC50 and pKd values of 7.1 and 8.0 [1].
The BRPF (bromodomain and PHD finger-containing) family BRPF1, BRPF2/BRD1, and BRPF3 operate as scaffolds to assemble MYST-family histone acetyltransferases (HATs) complexes. BRPF1 is a component of complexes containing the MOZ/MORF transcriptional coactivators and links the catalytic HATs to the other subunits ING5 and hEAF6.8. BRPF1 is important for maintaining skeletal development and Hox gene expression in fish [1].
In the BROMOscan panel of 35 bromodomain binding assays, PFI 4 exhibited excellent BRPF1 potency with pKd value of 8.0 and excellent selectivity over other bromodomains. In a cellular protein interaction assay, PFI 4 displaced NanoLuc-tagged BRPF1 bromodomain from Halotagged
histone H3.3 and disrupted chromatin binding [1].
Reference:
[1]. Demont EH, Bamborough P, Chung CW, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett, 2014, 5(11): 1190-1195.
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