Bax channel blocker

- Overview
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    Background
    
    IC50: 0.52 μM in Bax assayBax channel blocker is an inhibitor of Bax-mediated mitochondrial cytochrome c release. In the cytosol, cytochrome c is found to form a complex with dATP, Apaf-1, and procaspase-9, which results in caspase 9 activation followed by downstream activation of other caspases, such as caspase 8, ultimately leading to the cell death. After caspase 8 cleavage, the 15.5 kDa C-terminal fragment of Bid interacts with Bak and Bax.In vitro: Bax channel blocker, a 3,6-dibromocarbazole derivative, was observed to inhibit cytochrome c releasing from mitochondria by Bax channel modulation. The monohydroxy analogue Bax channel blocker remained the unprecedented inhibition of Bax-induced cytochrome c release at 10 μM. The IC50 value of Bax channel blocker was determined to be 0.52 μM, indicating that Bax channel blocker was a Bax channel inhibitor as hypothesized. Moreover, in the liposome assay, Bax channel blocker showing significant inhibition (>65%) of cytochrome c release at 10 μM also demonstrated sub-micromolar IC50 value [1]. In vivo: So far, there is no animal in vivo study conducted for Bax channel blocker. Clinical trial: N/A
- Properties
  - Alternative Name
    
    1-(3,6-dibromocarbazol-9-yl)-3-piperazin-1-ylpropan-2-ol;dihydrochloride
    
    CAS Number
    
    335165-68-9
    
    Molecular Formula
    
    C19H21Br2N3O·2HCl
    
    Molecular Weight
    
    540.12
    
    Appearance
    
    White solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥28.2 mg/mL in DMSO with ultrasonic; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Desiccate at RT
    
    * For Research Use Only

Bax channel blocker

Background

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