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LSN3154567 (also known as Nampt-IN-1) is a potent and elective NAMPT inhibitor, inhibits purified NAMPT with an IC50 of 3.1 nM. NAMPT is a promising antitumor target. NAMPT inhibition leads to attenuation of glycolysis, resulting in further perturbation of carbohydrate metabolism in cancer cells. LSN3154567 exhibits a broad spectrum of anticancer activity. To assess its anticancer activity, LSN3154567 is tested against a number of different types of cancer cell lines cultured in the absence or presence of nicotinic acid (NA) (10 μM). LSN3154567 exhibits a potent antiproliferative activity against many cell lines in the absence of NA. LSN3154567 exhibits a dose-dependent inhibition of NAD+ formation with estimated TED50 value of 2.0 mg/kg.
| Cell Experiment | |
|---|---|
| Cell lines | A2780 and KM-12, KMS-11 and MKN-74, OPM-2 and Kelly; and all other cancer cells |
| Preparation method | Cells are seeded in 96-well plates, cultured overnight, and treated with LSN3154567 (0.03 to 1,000 nM)±NA (10 μM) in duplicate at 37°C in 5% CO2 for 72 hours. Staurosporine (10 μM) is used as positive control. Cell viability is determined by a CytoTox-Glo Cytotoxicity assay kit. |
| Concentrations | 0.03 to 1,000 nM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 419.49 |
| Formula | C20H25N3O5S |
| CAS Number | 1698878-14-6 |
| Solubility (25°C) | DMSO: ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related NAMPT Products |
|---|
| JGB-1-155
JGB-1-155 is a positive allosteric modulators (N-PAMs), which enhances the activity of nicotinamide phosphoribosyltransferase NAMPT with EC50 of 3.29 μM. |
| Nampt activator-2
Nampt activator-2 is a potent NAMPT activator, with EC50 of 0.023 μM. |
| Teglarinad chloride
Teglarinad chloride (GMX1777) is a proagent of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). |
| NAMPT degrader-3
NAMPT degrader-3 is a NAMPT degrader, depending on VHL- and proteasome manner. |
| Nampt activator-3
NAMPT activator-3, a NAT derivative, is a NAMPT activator with an EC50 of 2.6 μM and a KD of 132 nM. |
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