Name: LY2409881
Price: 265.00 USD

- Overview
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    Background
    
    LY2409881 is a potent and selective inhibitor of IKK2 with IC50 value of 30 nM [1].
    IκB kinase β (IKK2) is an enzyme that serves as a subunit of IκB kinase, which is involved in the cytokine-activated immune responses. IKK2 activates nuclear factor kappa-B kinase (NF-κB).
    LY2409881 is a selective IKK2 inhibitor and exhibited >10-fold selectivity over other common kinases and IKK1. In the ovarian cancer cell line SKOV3, LY2409881 showed moderate cytotoxicity. While coadministration of LY2409881 and TNFɑ significantly induced cells death, which suggested LY2409881 inhibited NF-κB mediated antiapoptotic signals in a TNFɑ-dependent way. In the DLBCL cell line LY10, LY2409881 (10 μM) inhibited TNFɑ-dependent phosphorylation of IκB. In the DLBCL cell line SUDHL2, LY2409881 (10 μM) inhibited the nuclear signals of p50 and NF-κB. Also, LY2409881 induced apoptosis in a concentration-dependent way [1].
    In SCID-beige mice bearing LY10 cell-derived tumors, LY2409881 (50, 100 and 200 mg/kg) significantly inhibited tumor growth [1].
- Properties
  - Alternative Name
    
    2-(5-chloro-2-((3-(4-methylpiperazin-1-yl)propyl)amino)pyrimidin-4-yl)-N-cyclopropylbenzo[b]thiophene-4-carboxamide
    
    CAS Number
    
    946518-60-1
    
    Molecular Formula
    
    C24H32Cl4N6OS
    
    Molecular Weight
    
    594.43
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥59.4 mg/mL in DMSO with ultrasonic; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

LY2409881

LY2409881

Background

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