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LSN3154567

Cat. No. M9130
LSN3154567 Structure
Synonym:

Nampt-IN-1

Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 170  USD170 In stock
25mg USD 330  USD330 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Zhao G, et al. Mol Cancer Ther. Discovery of a Highly Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal Toxicity with Nicotinic Acid Coadministration.

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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.

Nampt-IN-8 

Nampt-IN-8 (Compound 10d) is an NAMPT inhibitor with an IC50 of 0.183 μM. Nampt-IN-8 is also a relatively good NQO1 substrate. Nampt-IN-8 induces cell apoptosis and ROS.

GNE-618 

GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity.

GPP78

GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects.

  Catalog
Abmole Inhibitor Catalog




Keywords: LSN3154567, Nampt-IN-1 supplier, NAMPT, inhibitors, activators


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