Name: CHIR-98014
Price: 273.00 USD

- Overview
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    Background
    
    CHIR-98014 is a potent inhibitor of GSK-3α and GSK-3β with IC50 values of 0.65 nM and 0.58 nM, respectively [1] GSK-3 (Glycogen synthase kinase 3) is a serine/threonine protein kinase and plays a pivotal role in a number of central intracellular signaling pathways, including cellular proliferation, migration, inflammation and immune responses, glucose regulation, and apoptosis. Recently, it has been reported that GSK-3 abnormally expressed in a variety of diseases, including Type II diabetes, Alzheimer's Disease, inflammation, cancer, and bipolar disorder [2, 3]. CHIR-98014 is a potent GSK-3α and GSK-3β inhibitor. When tested with insulin receptor-expressing CHO-IR cells or primary rat hepatocytes, CHIR-98014 stimulated the GS activity ratio as high as two- to three fold compared with basal in a dose dependent manner. Similarly, in isolated type 1 skeletal muscle from insulin-sensitive lean Zucker and from insulin-resistant ZDF rats, administration of CHIR-98014 activated GS activity ratio [1]. In mouse ES-D3 cells, CHIR-98014 treatment (48 and 72 hours later) resulted in a significant activation of the Wnt/beta-catenin pathway via inhibiting GSK-3 [4]. In markedly diabetic and insulin-resistant db/db mice model, oral administration of CHIR-98014 (30mg/kg) significantly reduced fasting hyperglycemia within 4 hours and improved glucose disposal during an ipGTT [1].
    
    [1]. Ring, D.B., et al., Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes, 2003. 52(3): p. 588-95.
    [2]. Pan WA, et al. The RNA recognition motif of NIFK is required for rRNA maturation during cell cycle progression. RNA Biol. 2015. 12(3):255-67.
    [3]. McCubrey JA, et al. GSK-3 as potential target for therapeutic intervention in cancer. Oncotarget. 2014. 5(10):2881-911.
    [4]. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors. BMC Res Notes. 2014. 7(1):273-281.
- Properties
  - Alternative Name
    
    6-N-[2-[[4-(2,4-dichlorophenyl)-5-imidazol-1-ylpyrimidin-2-yl]amino]ethyl]-3-nitropyridine-2,6-diamine
    
    CAS Number
    
    252935-94-7
    
    Molecular Formula
    
    C20H17Cl2N9O2
    
    Molecular Weight
    
    486.31
    
    Appearance
    
    A solid
    
    Purity
    
    99.13%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥8.1 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CHIR-98014

CHIR-98014

Background

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