CHS-828

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP15158CAS No. ：200484-11-3Purity：98%

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CAS No.	200484-11-3	Cat. No.	BCP15158
Name	CHS-828
Synonyms	CHS828;CHS 828;GMX1778;GMX-1778;GMX 1778;
SMILES
Chemical Name
Formula	C19H22ClN5O	M. Wt	371.87
Purity	98%	Storage	Store at 4-8°C
Description	in vitro: The phosphoribosyltransferase activity of recombinant NAMPT was sensitive to inhibition by GMX1778 (IC50 < 25 nM) whereas the adenyltransferase activity of recombinant NMNAT1 was not. The Kd of recombinant NAMPT for GMX1778 labeled with a fluorescent tag (GMX1778-Alexa Fluor) was 120 nM. Overexpression of wild-type NAMPT was able to maintain a certain level of NAD+ under conditions of challenge with 3 nM GMX1778, but this effect was lost when cells were exposed to 300 nM GMX1778 . GMX1778 increases intracellular ROS in cancer cells by elevating the superoxide level while decreasing the intracellular NAD(+) level. Notably, GMX1778 treatment does not induce ROS in normal cells. GMX1778-induced ROS can be diminished by adding nicotinic acid (NA) in a NA phosphoribosyltransferase 1 (NAPRT1)-dependent manner . in vivo: A 4-h iv infusion of NA (120 mg/kg of body weight) did not adversely affect the antitumor activity of a 24-h iv infusion of GMX1777 at a dose of 150 mg/kg or 650 mg