| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P422232-1ml |
1ml |
现货  |
|
| 别名 | (E)-1-(2-羟基苯基)-3-((1R,4R)-5-(吡啶-2-基)-2,5-二氮杂双环[2.2.1]庚-2-基)丙酸酯-2-en-1-酮 |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | PFI-3 |
| 生化机理 | Polybromo（Kd = 48 nM）和SMARCA4（K d = 89 \ xa0nM）的有效和选择性抑制剂。还抑制SMARCA2。对家族VIII溴结构域显示高特异性。PFI-3对多种其他激酶具有选择性。 |
| 储存温度 | 避光,-80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 多溴 1 抑制剂；SWI/SNF 相关抑制剂；基质相关；染色质的肌动蛋白依赖性调节剂；a 亚家族；成员 4 |
| 产品介绍 |
PFI 3是有效的polybromo 1和SMARCA4选择性抑制剂，Kd值分别为48和89 nM。 转录激活剂BRG1（SMARCA4）是SWI/SNF家族成员，可调控转录。蛋白polybromo-1（PB1、PBRM1）是BRG1相关因子和肿瘤抑制子。 PFI 3是一种有效的polybromo 1和SMARCA4选择性抑制剂。PFI 3可结合SMARCA2和SMARCA4 bromodomains，Kd值分别为55和110 nM。PFI-3（2 μM）可抑制70%的PBRM1。在基于细胞的染色质结合试验中，PFI-3可以剂量依赖的方式替换GFP标记的SMARCA2，IC50值为5.78 μM。PFI-3是适用于研究SMARCA2/4 bromodomains的细胞通透性探针。在SMARCA4缺陷的A549、H1299和H157细胞系中，PFI-3不具有抗增殖功能，且不能从染色质中替换SMARCA2。在THP-1和MV4-11白血病细胞中，PFI 3不能诱导抗癌表型。 PFI-3是一个SMARCA bromodomains的选择性化学探针，包括SMARCA2, SMARCA4以及PB1(5) bromodomains。 Shipped at 4°C. Store at -20°C. Store In the Dark. |
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| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
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| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | (E)-1-(2-hydroxyphenyl)-3-[(1R,4R)-5-pyridin-2-yl-2,5-diazabicyclo[2.2.1]heptan-2-yl]prop-2-en-1-one |
| INCHI | InChI=1S/C19H19N3O2/c23-17-6-2-1-5-16(17)18(24)8-10-21-12-15-11-14(21)13-22(15)19-7-3-4-9-20-19/h1-10,14-15,23H,11-13H2/b10-8+/t14-,15-/m1/s1 |
| InChi Key | INAICWLVUAKEPB-QSTFCLMHSA-N |
| Canonical SMILES | C1C2CN(C1CN2C3=CC=CC=N3)C=CC(=O)C4=CC=CC=C4O |
| Isomeric SMILES | C1[C@@H]2CN([C@H]1CN2C3=CC=CC=N3)/C=C/C(=O)C4=CC=CC=C4O |
| PubChem CID | 78243717 |
| MeSH Entry Terms | PF-06687252;PFI-3 compound |
| 分子量 | 321.4 |
| 分子量 | 321.400 g/mol |
|---|---|
| XLogP3 | 3.300 |
| 氢键供体数Hydrogen Bond Donor Count | 1 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 4 |
| 精确质量Exact Mass | 321.148 Da |
| 单同位素质量Monoisotopic Mass | 321.148 Da |
| 拓扑极表面积Topological Polar Surface Area | 56.700 Ų |
| 重原子数Heavy Atom Count | 24 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 495.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 2 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 1 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 1 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Yellow-green Liquid) | Pass |
| Record the entire process by video | Conform |
| 1. Xuan Ren, Jianchun Xu, Qingsong Xue, Yi Tong, Tairan Xu, Jinli Wang, Ting Yang, Yuan Chen, Deshun Shi, Xiangping Li. (2024) BRG1 enhances porcine iPSC pluripotency through WNT/β-catenin and autophagy pathways. THERIOGENOLOGY, 215 (22): (10). [PMID:38000125] [10.1016/j.theriogenology.2023.11.014] |
| 2. Ren Xuan, Huang Shihai, Xu Jianchun, Xue Qingsong, Xu Tairan, Shi Deshun, Ma Shinan, Li Xiangping. (2024) BRG1 improves reprogramming efficiency by enhancing glycolytic metabolism. CELLULAR AND MOLECULAR LIFE SCIENCES, 81 (1): (1-14). [PMID:39643758] [10.1007/s00018-024-05527-2] |
| 1. Xuan Ren, Jianchun Xu, Qingsong Xue, Yi Tong, Tairan Xu, Jinli Wang, Ting Yang, Yuan Chen, Deshun Shi, Xiangping Li. (2024) BRG1 enhances porcine iPSC pluripotency through WNT/β-catenin and autophagy pathways. THERIOGENOLOGY, 215 (22): (10). [PMID:38000125] [10.1016/j.theriogenology.2023.11.014] |
| 2. Ren Xuan, Huang Shihai, Xu Jianchun, Xue Qingsong, Xu Tairan, Shi Deshun, Ma Shinan, Li Xiangping. (2024) BRG1 improves reprogramming efficiency by enhancing glycolytic metabolism. CELLULAR AND MOLECULAR LIFE SCIENCES, 81 (1): (1-14). [PMID:39643758] [10.1007/s00018-024-05527-2] |
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