Name: SGI-1027
Price: 281.00 USD

- Overview
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    Background
    
    SGI-1027 is an inhibitor of DNMT with IC50 values of 12.5μM, 8μM and 7.5μM, respectively for DNMT1, DNMT3A and DNMT3B [1].SGI-1027 shows inhibition with mammalian DNMTs and bacterial M. SssI in vitro. Both the endogenous and recombinant DNMTs can be inhibited by SGI-1027. The mechanism of this inhibition is that SGI-1027 competes with Ado-Met but not the substrate DNA within the cofactor binding site of the enzyme. SGI-1027 inhibits DNA methylation through directly inhibiting DNMTs [1].In cancer cells, many TSGs are silenced due to hypermethylation of CpG islands in their promoters. SGI-1027 can demethylates these CpG islands and reactivate the silenced TSGs. In RKO cells, prolonged treatment of SGI-1027 induces reexpression of P16 and TIMP3 genes. Moreover, SGI-1027 is found to cause selective degradation of DNMT1 via proteasomal pathway [1].
    
    [1] Datta J, Ghoshal K, Denny WA, Gamage SA, Brooke DG, Phiasivongsa P, Redkar S, Jacob ST. A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. Cancer Res. 2009 May 15;69(10):4277-85.
- Properties
  - Alternative Name
    
    N-[4-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl]-4-(quinolin-4-ylamino)benzamide
    
    CAS Number
    
    1020149-73-8
    
    Molecular Formula
    
    C27H23N7O
    
    Molecular Weight
    
    461.52
    
    Appearance
    
    A solid
    
    Purity
    
    98.60%
    
    Solubility
    
    ≥22.25 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Ryan Richards, Megan E. Honeywell, et al. "FLICK: an optimized plate reader-based assay to infer cell death kinetics." STAR Protoc. 2021 Feb 3;2(1):100327. PMID:33659903