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PFI 4
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PFI 4图片
CAS NO:900305-37-5
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)询价
10mg询价
50mg询价

PFI 4 (compound 11) 是一种有效且高度选择性的 BRPF1 Bromodomain (BRPF1B) 抑制剂，IC50 为 172 nM。 PFI 4 可用于探索 HBO1/BRPF1 复合物的功能机制，并研究骨质流失和溶骨性恶性骨病变。
Cas No.900305-37-5
化学名N-(1,3-dimethyl-2-oxo-6-(pyrrolidin-1-yl)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide
Canonical SMILES[H]N(C(C1=CC=CC=C1OC)=O)C2=C(N3CCCC3)C=C(N(C)C(N4C)=O)C4=C2
分子式C21H24N4O3
分子量380.44
溶解度≥ 13.3mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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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