CHS-828 (nicotinate)
CHS-828 nicotinate is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 nicotinate (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD+ and exhibits a potent anticancer activity[1].
Product Specifications
CAS Number
1160589-73-0
Product Name Alternative
GMX1778 (nicotinate)
UNSPSC
12352005
Target
Apoptosis; NAMPT
Type
Reference compound
Related Pathways
Apoptosis; Metabolic Enzyme/Protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/chs-828-nicotinate.html
Smiles
N#CN/C(NCCCCCCOC1=CC=C(C=C1)Cl)=N\C2=CC=NC=C2.O=C(C3=CC=CN=C3)O
Molecular Formula
C25H27ClN6O3
Molecular Weight
494.97
References & Citations
[1]Watson M, et al. The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors. Mol Cell Biol. 2009 Nov;29 (21) :5872-88.|[2]Cerna D, et al. Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by small molecule GMX1778 regulates reactive oxygen species (ROS) -mediated cytotoxicity in a p53- and nicotinic acid phosphoribosyltransferase1 (NAPRT1) -dependent manner. J Biol Chem. 2012 Jun 22;287 (26) :22408-17.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 1
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