NSC 687852 (b-AP15)

- Overview
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    Background
    
    IC50: N/ANSC 687852 is a 19S regulatory particle inhibitor. The 19S particles bind polyubiquitin-linked polypeptides and present them to the 20S degradative units. USP14 and UCHL5 are cysteine enzymes that become activated after being associated with the proteasome.In vitro: NSC 687852 blocked deubiquitylating activity of USP14 and UCHL5 selectively without inhibiting proteasome activity. NSC 687852 decreased viability in multiple myeloma (MM) cell lines and patient MM cells, inhibited MM cell proliferation even in the presence of bone marrow stroma cells, and overcomed bortezomib resistance. Anti-MM activity of NSC 687852 was associated with growth arrest through downregulating CDC2, CDC25C, and cyclin B1, as well as induction of caspase-dependent apoptosis and activation of unfolded protein response [1]. In vivo: In vivo studies using distinct human MM xenograft models showed that NSC 687852 was well tolerated, inhibited tumor growth, and prolonged mouse survival. Combination of NSC 687852 with suberoylanilide hydroxamic acid, lenalidomide, or dexamethasone was found to induce synergistic anti-MM activity [1]. Clinical trial: N/A
- Properties
  - Alternative Name
    
    b-AP15; (3E,5E)-3,5-bis[(4-nitrophenyl)methylidene]-1-prop-2-enoylpiperidin-4-one
    
    CAS Number
    
    1009817-63-3
    
    Molecular Formula
    
    C22H17N3O6
    
    Molecular Weight
    
    419.39
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥20.95 mg/mL in DMSO
    
    Storage
    
    Store at 4°C
    
    * For Research Use Only

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NSC 687852 (b-AP15)

Background

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