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TCS PIM-1 1Pim-1 kinase inhibitor,ATP-competitve

TCS PIM-1 1

Catalog No. A4521
Size Price Stock Qty
10mM (in 1mL DMSO) $119.00 In stock
10mg $108.00 In stock
50mg $470.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

TCS PIM-1 1

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Chemical Properties

Cas No. 491871-58-0 SDF Download SDF
Chemical Name 6-(5-bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydropyridine-3-carbonitrile
Canonical SMILES O=C1C(C#N)=C(C2=CC=CC=C2)C=C(C3=C(O)C=CC(Br)=C3)N1
Formula C18H11BrN2O2 M.Wt 367.2
Solubility >12.8mg/mL in DMSO Storage Store at 4°C
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Background

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.