K-7174

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Description:
    IC50: 9 μM
    The main function of the proteasome is to degrade unneeded or damaged proteins by proteolysis, a chemical reaction that breaks peptide bonds. Proteasome inhibition is now considered a unique and effective way to kill cancer cells that can tolerate conventional chemotherapy. K-7174 is a novel orally active proteasome inhibitor.
    In vitro: Due to its proteasome inhibitary effect, K-7174 induces transcriptional repression of class I histone deacetylases (HDAC) via caspase-8-dependent degradation of Sp1, the most potent transactivator of class I HDAC genes. HDAC1 overexpression reduces the cytotoxic effect of K-7174 and abrogates histone hyperacetylation without affecting the ubiquitinated protein accumulation in K-7174-treated myeloma cells [1].
    In vivo: K-7174 exhibits the therapeutic effects through its anti-proteasome activities, which is stronger when administered orally than intravenously, without obvious side effects in a murine myeloma model. In addition, K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib [1].
    Clinical trial: Up to now, K-7174 is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    1,4-bis((E)-5-(3,4,5-trimethoxyphenyl)pent-4-en-1-yl)-1,4-diazepane dihydrochloride
    
    CAS Number
    
    191089-60-8
    
    Molecular Formula
    
    C33H50Cl2N2O6
    
    Molecular Weight
    
    641.67
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥64.2 mg/mL in H2O; ≥51.6 mg/mL in EtOH; ≥61.8 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Martinez-H?yer S, Deng Y, et al. "Loss of lenalidomide-induced megakaryocytic differentiation leads to therapy resistance in del(5q) myelodysplastic syndrome." Nat Cell Biol. 2020;22(5):526-533. PMID:32251398

K-7174

Background

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