CHS-828

• CAT Number: I002539
• CAS Number: 200484-11-3
• Molecular Formula: C₁₉H₂₂ClN₅O
• Molecular Weight: 371.86
• Purity: ≥95%
• Target: Nampt
• Solubility: DMSO: ≥ 39 mg/mL
• Storage: Store at -20°C
• IC50: < 25 nM
• IUPAC Name: 2-[6-(4-chlorophenoxy)hexyl]-1-cyano-3-pyridin-4-ylguanidine
• InChI: InChI=1S/C19H22ClN5O/c20-16-5-7-18(8-6-16)26-14-4-2-1-3-11-23-19(24-15-21)25-17-9-12-22-13-10-17/h5-10,12-13H,1-4,11,14H2,(H2,22,23,24,25)
• InChIKey: BOIPLTNGIAPDBY-UHFFFAOYSA-N
• SMILES: C1=CC(=CC=C1OCCCCCCN=C(NC#N)NC2=CC=NC=C2)Cl

GMX1778（Cat No.:I002539）, also known as CHS828, is a highly potent and selective inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). With an IC50 of less than 25nM and a Kd of 120nM, it effectively inhibits NAMPT activity. GMX1778 has shown the ability to induce programmed cell death with characteristic features of apoptosis. By targeting NAMPT, an enzyme involved in nicotinamide adenine dinucleotide (NAD+) biosynthesis, GMX1778 disrupts cellular energy metabolism, leading to cell death. These properties highlight the potential of GMX1778 as an anticancer agent with apoptotic-inducing properties.

Reference

1:NAMPT Inhibitor GMX1778 Enhances the Efficacy of 177Lu-DOTATATE Treatment of Neuroendocrine Tumors. Elf AK, Bernhardt P, Hofving T, Arvidsson Y, Forssell-Aronsson E, Wängberg B, Nilsson O, Johanson V.J Nucl Med. 2017 Feb;58(2):288-292. doi: 10.2967/jnumed.116.177584. Epub 2016 Sep 29. PMID: 27688470 2: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. Cerna D, Li H, Flaherty S, Takebe N, Coleman CN, Yoo SS.J Biol Chem. 2012 Jun 22;287(26):22408-17. doi: 10.1074/jbc.M112.357301. Epub 2012 May 8. PMID: 22570471 Free PMC Article3:The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors. Watson M, Roulston A, Bélec L, Billot X, Marcellus R, Bédard D, Bernier C, Branchaud S, Chan H, Dairi K, Gilbert K, Goulet D, Gratton MO, Isakau H, Jang A, Khadir A, Koch E, Lavoie M, Lawless M, Nguyen M, Paquette D, Turcotte E, Berger A, Mitchell M, Shore GC, Beauparlant P.Mol Cell Biol. 2009 Nov;29(21):5872-88. doi: 10.1128/MCB.00112-09. Epub 2009 Aug 24. PMID: 19703994 Free PMC Article