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GMX1778

Chemical Structure : GMX1778

CAS No.: 200484-11-3

GMX1778 (CHS-828;GMX-1778)

Catalog No.: PC-42257Not For Human Use, Lab Use Only.

GMX1778 (CHS-828) is a potent, specific, competitive NAMPT inhibitor with Kd of 120 nM, enzyme IC50 of <25 nM.

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Biological Activity

GMX1778 (CHS-828) is a potent, specific, competitive NAMPT inhibitor with Kd of 120 nM, enzyme IC50 of <25 nM.
GMX1778 blocks the NAD+ biosynthesis and results in tumor cell death, furthermore, phosphoribosylated by NAMPT, increases its cellular retention.
GMX1778 also induces ROS in cancer cells, but not in normal cells.
The prodrug of GMX1778, GMX1777, shows antitumor activity in vivo combined with nicotinic acid.

Physicochemical Properties

M.Wt 371.8639
Formula C19H22ClN5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 39 mg/mL

Chemical Name/SMILES

Guanidine, N-[6-(4-chlorophenoxy)hexyl]-N'-cyano-N''-4-pyridinyl-

References

1. Watson M, et al. Mol Cell Biol. 2009 Nov;29(21):5872-88.

2. Jonsson E, et al. Cancer Lett. 2001 Jan 26;162(2):193-200.

3. Hjarnaa PJ, et al. Cancer Res. 1999 Nov 15;59(22):5751-7.

4. Cerna D, et al. J Biol Chem. 2012 Jun 22;287(26):22408-17.

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