CHS-828

CHS-828 (GMX1778) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD+ and exhibits a potent anticancer activity[1].

Product Specifications

CAS Number

[200484-11-3]

Product Name Alternative

GMX1778

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; NAMPT

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GMX1778.html

Purity

99.28

Solubility

DMSO : ≥ 39 mg/mL

Smiles

N#CN/C(NCCCCCCOC1=CC=C(C=C1)Cl)=N\C2=CC=NC=C2

Molecular Formula

C19H22ClN5O

Molecular Weight

371.86

Precautions

H302, H315, H319, H335

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.