化学信息：
| 化学名 | N-(1,3-dimethyl-2-oxo-6-pyrrolidin-1-ylbenzimidazol-5-yl)-2-methoxybenzamide |
|
| 简称 | PFI-4 | |
| 别名 |
PFI4, PFI 4 |
|
| 中文名 | N/A | |
| 化学式 | C21H24N4O3 | |
| 分子量 | 380.44 | |
| CAS号 | 900305-37-5 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO17mg/ml warming; Ethanol5mg/ml warming |
|
| 溶液配制 | 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。 |
生物信息：
| 产品描述 | PFI-4是一种有效的选择性BRPF1 bromodomain抑制剂，IC50为80nM。 | ||||
| 信号通路 | Epigenetics | ||||
| 靶点 | BRPF1 | BRPF2 | BRPF3 | － | － |
| IC50 | 80nM | 7.9μM | >10μM | － | － |
| 体外研究 | PFI-4 is cell permeable, and acts by displacing the BRPF1 bromodomain from Histone H3.3. | ||||
| 体内研究 | N/A | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
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)：
| 酶活性检测实验 | |
| 方法 | 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. |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SD1141-10mM | PFI-4 (Epigenetic Reader Domain抑制剂) | 10mM×0.2ml |
| SD1141-5mg | PFI-4 (Epigenetic Reader Domain抑制剂) | 5mg |
| SD1141-25mg | PFI-4 (Epigenetic Reader Domain抑制剂) | 25mg |
| — | 说明书 | 1份 |
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。
