A Pim-1 kinase inhibitor
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].
参考文献:
[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.
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