| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G421275-1ml |
1ml |
现货  |
|
| 英文别名 | AC-29016 | 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone | Ethanone, 1-(5-(4-amino-7-methyl-7H-pyrrolo(2,3-d)pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl)-2-(3-(trifluoromethyl)phenyl)- | 1-[5-(4-a |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | GSK2606414 |
| 生化机理 | 有力和选择性的蛋白激酶R样ER激酶（PERK）抑制剂（IC50 = 0.4 nM）。与HR1和PKR相比，PERK具有> 1000倍的选择性。抑制thapsigargin诱导的肺癌A549细胞中的PERK磷酸化。减轻小鼠中皮下胰腺人类肿瘤异种移植物的生长。口服具有生物活性。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 产品介绍 |
GSK2606414是口服活性的PERK高活性抑制剂，IC50为0.4 nM。 GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | 1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone |
| INCHI | 1S/C24H20F3N5O/c1-31-12-18(21-22(28)29-13-30-23(21)31)15-5-6-19-16(11-15)7-8-32(19)20(33)10-14-3-2-4-17(9-14)24(25,26)27/h2-6,9,11-13H,7-8,10H2,1H3,(H2,28,29,30) |
| InChi Key | SIXVRXARNAVBTC-UHFFFAOYSA-N |
| Smiles | CN1C=C(C2=C(N=CN=C21)N)C3=CC4=C(C=C3)N(CC4)C(=O)CC5=CC(=CC=C5)C(F)(F)F |
| Isomeric SMILES | CN1C=C(C2=C(N=CN=C21)N)C3=CC4=C(C=C3)N(CC4)C(=O)CC5=CC(=CC=C5)C(F)(F)F |
| 分子量 | 451.44 |
| Reaxy-Rn | 21981831 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21981831&ln= |
| 分子量 | 451.400 g/mol |
|---|---|
| XLogP3 | 3.800 |
| 氢键供体数Hydrogen Bond Donor Count | 1 |
| 氢键受体数Hydrogen Bond Acceptor Count | 7 |
| 可旋转键计数Rotatable Bond Count | 3 |
| 精确质量Exact Mass | 451.162 Da |
| 单同位素质量Monoisotopic Mass | 451.162 Da |
| 拓扑极表面积Topological Polar Surface Area | 77.000 Ų |
| 重原子数Heavy Atom Count | 33 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 721.000 |
| 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 | 0 |
| 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 | 0 |
| 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 | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 1. Xiaohua Xie, Xiaofeng Wu, Dongsheng Zhao, Ying Liu, Qiyue Du, Yitian Li, Yaping Xu, Yuhang Li, Yan Qiu, Yungang Yang. (2023) Fluvoxamine alleviates bleomycin-induced lung fibrosis via regulating the cGAS-STING pathway. PHARMACOLOGICAL RESEARCH, 187 (106577). [PMID:36435270] [10.1016/j.phrs.2022.106577] |
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