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TCS PIM-1 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TCS PIM-1 1图片
CAS NO:491871-58-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
TCS PIM-1 1 (SC 204330) 是一种有效的、选择性的和 ATP 竞争性的 Pim-1 激酶抑制剂,IC50 为 50 nM,比 Pim-2 和 MEK1/MEK2 具有良好的选择性 (IC50s >20000 nM)。
Cas No.491871-58-0
别名SC 204330
化学名6-(5-bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydropyridine-3-carbonitrile
Canonical SMILESO=C1C(C#N)=C(C2=CC=CC=C2)C=C(C3=C(O)C=CC(Br)=C3)N1
分子式C18H11BrN2O2
分子量367.2
溶解度≥ 12.8mg/mL in DMSO
储存条件Store at 4℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

TCS PIM-1 1 is a selective inhibitor of Pim-1 with IC50 value of 50 nM [1].

Pim-1 is a proto-oncogene serine/threonine-protein kinase and plays an important role in cell cycle progression, apoptosis, transcriptional activation and more general signal transduction pathways. It has been shown that Pim-1 over-expression is correlated with a variety of human cancers [2].

TCS PIM-1 1 is a potent Pim-1 inhibitor and has a better selectivity to Pim-1 than to Pim-2. It was revealed that TCS PIM-1 1 was the most potent inhibitor of Pim-1 by outlining the crystal structure and it was also shown that TCS PIM-1 1 had better inhibitory activity to Pim-1 compared with Pim-2 [1].

References:
[1].  Cheney, I.W., et al., Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett, 2007. 17(6): p. 1679-83.
[2].   Cen, B., et al., The Pim-1 protein kinase is an important regulator of MET receptor tyrosine kinase levels and signaling. Mol Cell Biol, 2014. 34(13): p. 2517-32.