
簡要描述:TCS PIM-1 1 491871-58-0TCS PIM-1 1 is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).
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Product Category詳細(xì)介紹
| 品牌 | absin | CAS | 491871-58-0 |
|---|---|---|---|
| 分子式 | C18H11BrN2O2 | 純度 | 98% |
| 分子量 | 367.2 | 貨號 | abs47027964 |
| 規(guī)格 | 10mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a potent | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
TCS PIM-1 1 491871-58-0
| 產(chǎn)品描述 | |
| 描述 | TCS PIM-1 1 is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM). |
| 純度 | 98% |
| 儲存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | SC 204330 |
| 可溶性/溶解性 | DMSO : 100 mg/mL (272.33 mM; Need ultrasonic) |
| 生物活性 | |
| 靶點(diǎn) | Pim |
| In vitro(體外研究) | TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein. |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | CancerOncoproteins/suppressorsOncoproteinsSignal transducers CancerSignal transductionProtein phosphorylationSerine/threonine kinasesOther EpigeneticsChromatin RemodelingPolycomb SilencingOther NeuroscienceProcesses Signal TransductionProtein PhosphorylationSer / Thr KinasesOther Kinases Stem CellsHematopoietic ProgenitorsIntracellular Molecules Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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