BAM7

- Overview
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    Background
    
    BAM7 is a direct and selective activator of BAX with IC50 value of 3.3uM [1].In the competitive fluorescence polarization assay (FPA), BAM7 competes with FITC–BIM SAHB for BAX binding site(BH3) in a dose dependent manner. BAM7 shows no antiapoptotic or BAKΔC competitive binding interactions even at 50 μM dosing, revealing a remarkable selectivity of BAM7 for BAX. The interaction between BAM7 and BAX at the very surface induces the characteristic structural changes that yield functional BAX oligomerization. In the in vitro assay, BAM7 induces BAX-dependent cell death but not the cells with BAK. BAM7 could be developed to a new generation of apoptotic modulators that directly activate BCL-2 family executioner proteins in cancerand other diseases driven by pathologic apoptotic blockades [1].
    
    [1] Evripidis Gavathiotis, Denis E Reyna, Joseph A Bellairs, Elizaveta S Leshchiner, and Loren D Walensky. Direct and selective small-molecule activation of proapoptotic BAX. Nat Chem Biol. 2012 July ; 8(7): 639–645.
- Properties
  - Categories
    
    BAX activator, direct and selective
    
    Alternative Name
    
    BAM 7;BAM-7; (4E)-4-[(2-ethoxyphenyl)hydrazinylidene]-5-methyl-2-(4-phenyl-1,3-thiazol-2-yl)pyrazol-3-one
    
    CAS Number
    
    331244-89-4
    
    Molecular Formula
    
    C21H19N5O2S
    
    Molecular Weight
    
    405.47
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    Limited solubility, soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CCOC1=CC=CC=C1NN=C2C(=NN(C2=O)C3=NC(=CS3)C4=CC=CC=C4)C
    
    * For Research Use Only