3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone

Uses

TCS PIM-1 1 is a Pim-1 kinase inhibitor.

Definition

ChEBI: 3-cyano-4-phenyl-6-(3-bromo-6-hydroxyphenyl)-2-pyridone is a member of the class of pyridones that is 2-pyridone carrying cyano, phenyl and 3-bromo-6-hydroxyphenyl substituents at positions 3, 4 and 6 respectively It is a pyridone, a bromophenol and a nitrile.

Biological Activity

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].

storage

Store at +4°C

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.