Name: JW 74
Price: 277.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: 790 nM for canonical Wnt signaling JW 74 is an inhibitor of the catalytic PARP domain of TNKS1/2.Wnt/β-catenin, a major regulator of stem cell self-renewal and differentiation, is aberrantly activated in a several cancers, including osteosarcoma. Thus, attenuation of Wnt/β-catenin activity by tankyrase inhibitors is an appealing strategy in osteosarcoma treatment.In vitro: Previous study found that JW74 at the molecular level induced stabilization of AXIN2, a key component of the β-catenin destruction complex, leading to reduced levels of nuclear β-catenin. In addition, JW74 could induce reduced cell growth in all tested cell lines, partially due to a delay in cell cycle progression and partially because of an induction of caspase-3-mediated apoptosis. Moreover, JW74 was able to induce the differentiation in U2OS cells and also enhance differentiation of OS cell lines that did not harbor a differentiation block [1]. In vivo: Previous animal study found that the dose of 150 mg/kg of JW74 in ApcMin model could reduce the small intestinal adenoma by 48% and was comparable with celecoxib or rofecoxib. Furthermore, it was noteworthy that JW74 became rapidly cleared from the blood stream due to its poor in vivo stability [2]. Clinical trial: Up to now, JW 74 is still in the preclinical development stage.
    
    1. E. W. Stratford, J. Daffinrud, E. Munthe, et al. The tankyrase-specific inhibitor JW74 affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines. Cancer Med. 3(1), 36-46 (2014).2. Waaler J et al. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011 Jan 1;71(1):197-205.
- Properties
  - Alternative Name
    
    4-[4-(4-methoxyphenyl)-5-[[[3-(4-methylphenyl)-1,2,4-oxadiazol-5-yl]methyl]thio]-4H-1,2,4-triazol-3-yl]-pyridine
    
    CAS Number
    
    863405-60-1
    
    Molecular Formula
    
    C24H20N6O2S
    
    Molecular Weight
    
    456.5
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

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