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CHS-828 (GMX1778) is a potent and specific inhibitor of NAMPT with IC50 and Kd value of <25 nM and 120 nM, respectively. CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome. GMX1778 induces NAD+ depletion through inhibition of NAD+ biosynthesis, followed by ATP depletion and ultimately resulted in cell death. GMX1778 suppresses nuclear factor-kappa B activity in cancer cells through downregulation of IKK activity (IC50=8 nM).
In vivo: GMX1778 (250 mg/kg, p.o.) shows marked antitumoural activity against three different human neuroendocrine tumours, midgut carcinoid (GOT1), pancreatic carcinoid (BON), and medullary thyroid carcinoma (GOT2), transplanted in nude mice.
| Cell Experiment | |
|---|---|
| Cell lines | HeLa cells |
| Preparation method | Serial dilutions of GMX1778 in DMSO are performed to achieve a final concentration of 0.2% DMSO. Relative ATP levels after 72 h are determined using a ViaLight HS high-sensitivity cytotoxicity and cell proliferation BioAssay kit per the manufacturer's instructions. For GMX1778 cytotoxicity rescue experiments, cells are treated with NA (10 μM) or NMN (100 μM) simultaneously with GMX1778. Sigmoidal dose-response curves are generated by nonlinear regression analysis of variable slope using GraphPad Prism version 4.00 (GraphPad Software) to calculate 50% inhibitory (IC50) values. |
| Concentrations | ~100 nM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Nude mice bearing midgut carcinoid (GOT1), pancreatic carcinoid (BON) and medullary thyroid cancer (GOT2) tumors |
| Formulation | Suspended in 2% carboxymethyl cellulose in 0.9% saline |
| Dosages | ~250 mg/kg |
| Administration | p.o. |
| Molecular Weight | 371.86 |
| Formula | C19H22ClN5O |
| CAS Number | 200484-11-3 |
| Solubility (25°C) | DMSO: ≥ 60 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 |
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STF-118804 is a highly specific NAMPT inhibitor. |
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P7C3 is an orally bioavailable and blood-brain barrier penetrant aminopropyl carbazole, with neuroprotective effects. P7C3 exerts its proneurogenic activity by protecting newborn neurons from apoptosis. P7C3 also enhances learning and memory in aged rats. |
| LSN3154567
LSN3154567 (also known as Nampt-IN-1) is a potent and elective NAMPT inhibitor, inhibits purified NAMPT with an IC50 of 3.1 nM. |
| GNE-617
GNE-617 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with IC50 value of 5nM. |
| SBI-797812
SBI-797812 is an activator of NAMPT that is structurally similar to active site-directed NAMPT inhibitors, preventing these inhibitors from binding to NAMPT. SBI-797812 transforms NAMPT into a "super catalyst" that generates NMN more efficiently. |
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