Name: GMX1778 (CHS828)
Price: 180.00 USD

- Overview
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    Background
    
    GMX1778 (CHS828) is a potent and specific inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with a Kd value of 120 nM [1].NAMPT is an NAD+ biosynthesis enzyme. NAD+ is a cofactor of enzymatic redox reactions that are involved in cellular metabolism, including ATP production. NAD+ is also important in many cellular pathways responsible for gene regulation, calcium homeostasis, genomic integrity, longevity and apoptosis. Cancer cells are significantly dependent on NAD+ for supporting high levels of ATP production for rapid cell proliferation [1]. Treatment with 30 nM GMX1778 for 6 h, extracts of IM-9 cells showed decreased NAD+ and NM levels, compared to cytosolic extracts of untreated cells. These levels continued to decrease throughout the rest of the time course experiment. The most profoundly changed was the metabolite NAD+ level. Between the 6- and 20-h time points, the decline of NAD+ occurred [1].The NAD+ salvage pathway produces NAD+ using either nicotinic acid (niacin) (NA) or nicotinamide (niacinamide) (NM) as a substrate. NAPRT1 is short for NA phosphoribosyltransferase 1. On xenograft tumors derived from NAPRT1-proficient (HCT-116) and NAPRT1-deficient (HT1080) cell lines in mice, a 24-h iv infusion of GMX1777 at 150 mg/kg or 650 mg/kg produced antitumor activity. A 4-h iv infusion of NA at 120 mg/kg did not adversely affect the antitumor activity of GMX1777 in the NAPRT1-deficient xenograft, but abolished the antitumor activity of GMX1777 against the NAPRT1-proficient HCT-116 cell line [1].
- Properties
  - Alternative Name
    
    (Z)-2-(6-(4-chlorophenoxy)hexyl)-1-cyano-3-(pyridin-4(1H)-ylidene)guanidine
    
    CAS Number
    
    200484-11-3
    
    Molecular Formula
    
    C19H22ClN5O
    
    Molecular Weight
    
    371.86
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥18.3 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only