LKB1 (AAK1 dual inhibitor)

- Overview
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    Background
    
    LKB1 is a selective inhibitor of Pim-1 kinase with Kd value of 35 nM [1].Pim-1 (proto-oncogene serine/threonine-protein kinase) is a proto-oncogene encodes by PIM1 gene and is reported to play an important role in multiple human cancers. Initially, pim-1 is reported to be expressed in spleen, thymus, bone marrow, prostate, oral epithelial cells, etc. Recently, the high expression of pim-1 has been identified in several isolated human cancer cells and been shown to involve in the cell cycle progression, apoptosis, transcriptional activation and many general signal transduction pathways. Therefore, investigation of the inhibition of pim-1 by low molecular weight compounds as a part of anticancer therapeutic strategies needs more attention and progress [2, 3].
    
    1. Bamborough, P., et al., Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. J Med Chem, 2008. 51(24): p. 7898-914.
    2. Natarajan, K., et al., The Pim kinase inhibitor SGI-1776 decreases cell surface expression of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and drug transport by Pim-1-dependent and -independent mechanisms. Biochem Pharmacol, 2013. 85(4): p. 514-24.
    3. Tsuganezawa, K., et al., A novel Pim-1 kinase inhibitor targeting residues that bind the substrate peptide. J Mol Biol, 2012. 417(3): p. 240-52.
- Properties
  - Alternative Name
    
    LKB1/AAK1 dual inhibitor; N-[5-(4-cyanophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyridine-3-carboxamide
    
    CAS Number
    
    1093222-27-5
    
    Molecular Formula
    
    C20H13N5O
    
    Molecular Weight
    
    339.36
    
    Purity
    
    99.01%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥34.8 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

LKB1 (AAK1 dual inhibitor)

Background

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