Name: YH239-EE
Price: 241.00 USD

- Overview
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    Background
    
    YH239-EE is a potent antagonist of p53-MDM2 [1].
    p53 is a transcription factor and functions as a tumor suppressor. MDM2 is a negative regulator of p53. The interaction of p53 and MDM2 has emerged as a novel target for anticancer drugs [1].
    YH239-EE is a potent p53-MDM2 antagonist. In OCI-AML-3 cells, YH239-EE potently inhibited cell proliferation. In AML cell lines, YH239-EE induced a cell cycle arrest and cell accumulation in the sub-G1 phase. YH239-EE induced apoptosis by 11.8-fold, 5.6-fold and 13.1-fold in OCI-AML-3, MOLM-13 and NB4 AML cell lines, respectively. In MOLM-13 cells, YH239 exhibited almost no apoptotic effect. However, YH239-EE significantly induced apoptosis. In MOLM-13 cells, (+)-YH239-EE and (−)-YH239-EE inhibited metabolic activity with EC50 values of 7.5 μM and 25.2 μM and induced apoptosis with 13.7% and 51.5% viable cells, respectively. (+)-YH239-EE (20 μM) induced p53 and significantly activated caspase 3 and 7 [1].
- Properties
  - Categories
    
    p53-MDM2 antagonist, potent
    
    Alternative Name
    
    (Z)-N-(tert-butyl)-2-(6-chloro-2-(ethoxycarbonyl)-1H-indol-3-yl)-2-(N-(4-chlorobenzyl)formamido)acetimidic acid
    
    CAS Number
    
    1364488-67-4
    
    Molecular Formula
    
    C25H27Cl2N3O4
    
    Molecular Weight
    
    504.41
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥50.4 mg/mL in DMSO; insoluble in H2O; ≥4.26 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Desiccate at -20°C
    
    SMILES
    
    CCOC(C1=C(C(N(C=O)CC2=CC=C(Cl)C=C2)/C(O)=N/C(C)(C)C)C3=C(N1)C=C(Cl)C=C3)=O
    
    * For Research Use Only