Name: ML216
Price: 212.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: 3.0 and 0.97 μM for full length BLM and BLM636–1298, respectivelyML216 is a potent inhibitor of the DNA unwinding activity of BLM helicase. BLM helicase is reported to be a DNA unwinding enzyme critical in DNA repair through the homologous recombination pathway. BLM gene mutations lead to diminished BLM helicase activity and can cause Bloom’s Syndrome. Similar to other DNA repair enzymes, BLM helicase inhibition shows sensitization of tumor cells to conventional cancer therapies, such as camptothecin.In vitro: ML216 showed submicromolar potency and selectivity over related helicases including RECQ1, RECQ5, and E. coli UvrD helicases. ML216 also inhibited cell proliferation of BLM-proficient fibroblast cells while had minimal effects on BLM deficient fibroblast cells, indicating on-target activity in a cellular context. Additionally, ML216 increased the frequency of sister chromatid exchanges, which was a diagnostic cellular phenotype consistent with the absence of a functional BLM protein [1]. In vivo: ML216 was a suitable starting point for further mouse tumor xenograft models and for the further development of potential cancer therapeutics [1]. Clinical trial: N/A
- Properties
  - Alternative Name
    
    1-(4-fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea
    
    CAS Number
    
    1430213-30-1
    
    Molecular Formula
    
    C15H9F4N5OS
    
    Molecular Weight
    
    383.32
    
    Appearance
    
    A solid
    
    Purity
    
    99.66%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥10.65 mg/mL in DMSO with gentle warming
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only

ML216

ML216

Background

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