Name: ACHP
Price: 444.00 USD

- Overview
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    Background
    
    IC50: 8.5 and 250 nM for IKKβ and IKKα, respectivelyACHP is an IκB kinase inhibitor. Nuclear factor-KB (NF-KB) involved in cell survival and proliferation of multiple myeloma has been well established. In vitro: ACHP is selective for IKKα and IKKβ over IKK3, Syk and MAPKKK4 (IC50 > 20 μM), DNA binding activity of NF-κB is inhibited. ACHP is an effective blockade NF-κB pathway in multiple myeloma cell lines, and induces cell growth arrest and apoptosis. It was observed that NF-KB is constitutively activated in all human myeloma cell lines, thus confirming the previous studies. In addition, It was found the phosphorylation of p65 subunit of NF-KB besides the phosphorylation of IKBA and the activation of NF-KB DNA binding and that various target genes of NF-KB including bcl-xL, XIAP, c-IAP1, cyclin D1, and IL-6 are up-regulated. 2-amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-piperidin-4-yl nicotinenitrile (ACHP) is a novel IKB kinase inhibitor. Treatment of myeloma cells with ACHP showed the cell growth was efficiently inhibited (IC50 values ranging from 18 to 35 Mmol/L) concomitantly with inhibition of the phosphorylation of IKBA/p65 and NF-KB DNA-binding, down-regulation of the NF-KB target genes, and then induction of apoptosis. In addition, the treatment of ACHP potentiated the cytotoxic effects of vincristine and melphalan (L-phenylalanine mustard), conventional antimyeloma drugs. These findings suggest that by blocking the antiapoptotic nature of myeloma cells endowed by the constitutive activation of NF-KB, IKB kinase inhibitors such as ACHP can sensitize myeloma cells to the cytotoxic effects of chemotherapeutic agents. In vivo: So far, no study in vivo has been conducted.Clinical trial: Clinical study has been conducted.
- Properties
  - Alternative Name
    
    (E)-2-amino-6-(2-(cyclopropylmethoxy)-6-oxocyclohexa-2,4-dien-1-ylidene)-4-(piperidin-4-yl)-1,6-dihydropyridine-3-carbonitrile
    
    CAS Number
    
    406208-42-2
    
    Molecular Formula
    
    C21H24N4O2
    
    Molecular Weight
    
    364.44
    
    Appearance
    
    Yellow solid
    
    Purity
    
    98.00%
    
    Solubility
    
    <7.29mg/ml in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

ACHP

ACHP

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