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merck millipore,默克密理博,516535,PERK Inhibitor I, GSK2606414 - CAS 1337531-89-1 - Calbiochem
产品名称：PERK Inhibitor I, GSK2606414 - CAS 1337531-89-1 - Calbiochem
产品型号：516535
The PERK Inhibitor I, GSK2606414 controls the biological activity of PERK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
merck millipore,默克密理博,516535,PERK Inhibitor I, GSK2606414 - CAS 1337531-89-1 - Calbiochem
- 产品介绍
重要规格表
经验配方 CAS号 C₂₄H₂₀F₃N₅O 1337531-89-1 描述 概述 A cell-permeable pyrrolopyrimidamine compound that acts as a highly potent EIF2AK3/PERK inhibitor (IC50 = 0.4 nM; [ATP] = 5 µM) by targeting PERK in its inactive DFG conformation at the ATP-binding region, while displaying ≥385-fold selectivity over c-Kit, Aurora B, BRK, HRI/EIF2AK1, MLK2/MAP3K10, c-MER, DDR2, PKR/EIF2AK2, and MLCK2/MYLK2 (IC50 = 154, 407, 412, 420, 452, 474, 524, 696, and 701 nM, respectively) and little activity against more than 280 other kinases (IC50 >1 µM). Shown to block ER stress-induced PERK autophosphorylation following Thapsigargin (Cat. No. 586005) addition in A549 cultures in vitro (by 100% at ≤30 nM; 60 min preincubation) and effectively retard PxBC-3 tumor growth in mice in vivo (50 and 150 mg/kg/12 h p.o.). Also available as a 25 mM solution in DMSO (Cat. No. 508340). 产品目录编号 516535 品牌系列 Calbiochem®
同义词 MERTK Inhibitor II, RP38 Inhibitor II, TAM Family RTK Inhibitor II, Double-stranded RNA-activated Protein Kinase Inhibitor II, Double-stranded RNA-dependent Protein Kinase Inhibitor II, DDR2 Inhibitor I, EIF2AK1 Inhibitor I, EIF2AK2 Inhibitor II, HRI Inhibitor I, MLCK Inhibitor VI, MLK2/MAP3K10 Inhibitor I, PKR-like ER Kinase Inhibitor I, Aurora Kinase Inhibitor IX, BRK Inhibitor I, c-Kit Inhibitor III, Mer RTK Inhibitor II, EIF2AK3 Inhibitor I, PKR Inhibitor II, 7-Methyl-5-(1-((3-trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, 1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone 参考 参考 Moreno, J.A., et al. 2013. Sci Transl. Med.<\\i> 5, 1.
Axten, J.M., et al. 2012. J. Med. Chem. 55, 7193.产品信息 CAS号 1337531-89-1 形式 White powder Hill配方 C₂₄H₂₀F₃N₅O Molar Mass 451.4 可逆 Y 结构配方图像 生物信息 主靶 Perk 主靶IC50 0.4 nM against EIF2AK3/PERK-catalyzed EIF2&alpha 纯度 ≥99% by HPLC 理化信息 细胞可渗透 Y 溶解度 DMSO 储存和货运信息 货运代码 Ambient Temperature Only
毒性 Standard Handling
储存 -20°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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