化学信息：
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化学名
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N-(1,3-dimethyl-2-oxo-6-pyrrolidin-1-ylbenzimidazol-5-yl)-2-methoxybenzamide
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简称
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PFI-4
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别名
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PFI4, PFI 4
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中文名
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N/A
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化学式
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C21H24N4O3
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分子量
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380.44
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CAS号
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900305-37-5
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO17mg/ml warming; Ethanol5mg/ml warming
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溶液配制
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5mg加入1.31ml DMSO，或者每3.8mg加入1ml DMSO，配制成10mM溶液。SD1141-10mM用DMSO配制。
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生物信息：
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产品描述
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PFI-4是一种有效的选择性BRPF1 bromodomain抑制剂，IC50为80nM。
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信号通路
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Epigenetics
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靶点
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BRPF1
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BRPF2
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BRPF3
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－
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－
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IC50
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80nM
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7.9μM
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>10μM
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－
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－
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体外研究
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PFI-4 is cell permeable, and acts by displacing the BRPF1 bromodomain from Histone H3.3.
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体内研究
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N/A
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临床实验
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N/A
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特征
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N/A
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相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
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酶活性检测实验
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方法
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Compounds are screened against 6H-Flag-Tev-BRPF1 (622-738), 6HisFlag-Tev-BRPF2 (also known as BRD1) (551-673) or 6His-Flag-Tev-BRPF3 (579-706) protein in dose-response format in a TR-FRET assay measuring competition between test compound and a synthetic fluorescent ligand. Compounds are titrated from 10mM in 100% DMSO and 100nl transferred to a low volume black 384 well micro titre plate using a Labcyte Echo 555. A Thermo Scientific Multidrop Combi is used to dispense 5μl of 4nM BRPF1, 20nM BRPF2 or 40nM BRPF3 protein respectively in an assay buffer of 50mM HEPES, 150mM NaCl, 5% glycerol, 1mM DTT and 1mM CHAPS, pH 7.4, and in the presence of the appropriate fluorescent ligand concentration (~Kd concentration for the interaction between protein and ligand). After equilibrating for 30 mins in the dark at rt, the bromodomain protein:fluorescent ligand interaction is detected using TR-FRET following a 5μl addition of either 3nM Lanthascreen Elite Tb-anti His antibody for the Alexa 488 ligands, or 3nM europium chelate labelled anti-6His antibody (Perkin Elmer, W1024, AD0111) for the Alexa 647 ligand, in assay buffer. Time resolved fluorescence energy transfer (TR-FRET) is then detected on a time-resolved fluorescence laser equipped Perkin Elmer Envision multimode plate reader using the appropriate protocol (excitation=337nM; emission 1 Alexa 488=495nM; emission 2 Alexa 488=520nM, emission 1 Alexa 647=615nM; emission 2 Alexa 647= 665nM ). TR-FRET ratio is calculated using the following equation: Ratio=((Acceptor fluorescence at 520 or 665nM) / (Donor fluorescence at 495 or 615nM)) * 1000. Data are analysed as for the BRD4 assay.
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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参考文献：
1. Demont EH, et al. ACS Med Chem Lett. 2014, 5(11), 1190-1195.
包装清单：
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产品编号
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产品名称
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包装
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SD1141-10mM
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PFI-4 (Epigenetic Reader Domain抑制剂)
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10mM×0.2ml
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SD1141-5mg
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PFI-4 (Epigenetic Reader Domain抑制剂)
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5mg
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SD1141-25mg
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PFI-4 (Epigenetic Reader Domain抑制剂)
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25mg
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—
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说明书
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1份
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保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
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