| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
2-NP targets STAT1 (signal transducer and activator of transcription 1), a transcription factor that plays a critical role in interferon signaling, immune responses, and tumor suppression. By selectively enhancing STAT1 transcription activity, 2-NP potentiates the effects of IFN-γ signaling. It prolongs IFN-γ-induced tyrosine phosphorylation of STAT1, which may underlie its ability to enhance STAT1-dependent transcription. Its selectivity for STAT1 over STAT3 and NF-κB supports its use as a specific probe for STAT1 function. 2-NP can enhance IFN-γ's ability to inhibit the proliferation of cancer cells.
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| ln Vitro |
In vitro, 2-NP is a selective enhancer of STAT1 transcription. It prolongs IFN-γ-induced tyrosine phosphorylation of STAT1, which may underlie its ability to enhance STAT1-dependent transcription. The compound enhances the ability of IFN-γ to inhibit the proliferation of human breast cancer and fibrosarcoma cells. Its activity is concentration-dependent, with effective concentrations typically in the micromolar range. Its selectivity for STAT1 over STAT3 and NF-κB makes it a valuable tool for studying STAT1 signaling, interferon responses, and cancer biology.
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| ln Vivo |
In vivo, 2-NP has been studied in a herpetic stromal keratitis (HSK) mouse model at a dose of 0.5 mg/kg via subconjunctival injection. Its ability to enhance STAT1 signaling may have therapeutic potential for viral infections and cancer. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying STAT1 signaling and interferon responses. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro STAT1 transcription activity assay for 2-NP typically uses cells transfected with a STAT1-responsive luciferase reporter construct. Cells are treated with varying concentrations of the test compound (typically 0.1 to 100 µM) and stimulated with IFN-γ. Luciferase activity is measured using a luminescence plate reader. STAT1 phosphorylation is assessed by Western blotting using phospho-STAT1 (Tyr701) antibodies. For selectivity profiling, the compound is tested against STAT3 and NF-κB reporter assays. Positive controls (e.g., known STAT1 activators) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, cancer cell lines (e.g., breast cancer, fibrosarcoma) are treated with 2-NP at concentrations ranging from 0.1 to 100 µM for 1-24 hours, with or without IFN-γ stimulation. STAT1 phosphorylation is assessed by Western blotting. STAT1 target gene expression (e.g., IRF1, CXCL10) is assessed by qRT-PCR. Cell viability is assessed using MTT or CellTiter-Glo assays. Proliferation is assessed by [³H]-thymidine incorporation or BrdU assays. All experiments include appropriate controls (vehicle, IFN-γ alone) and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, rodent models of viral infection or cancer are used. 2-NP is administered via subconjunctival injection, intraperitoneal injection, or oral gavage at doses ranging from 0.1 to 10 mg/kg. Disease severity is assessed by clinical scoring, viral load measurement, or tumor growth monitoring. All animal procedures should be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of 2-NP have been partially characterized. The compound has a molecular weight of 222.24 and a molecular formula of C14H10N2O. Following subconjunctival or intraperitoneal administration, the compound shows rapid absorption with a Tmax of 0.5-2 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including eye, liver, and kidney. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of 2-NP are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 10 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
2-NP is a selective STAT1 enhancer that prolongs IFN-γ-induced STAT1 phosphorylation. It enhances IFN-γ's ability to inhibit cancer cell proliferation. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥98%) for laboratory use only. Its selective STAT1 enhancement makes it a valuable tool for studying STAT1 signaling, interferon responses, and cancer biology.
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| Molecular Formula |
C14H10N2O
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|---|---|
| Molecular Weight |
222.242
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| Exact Mass |
222.079
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| CAS # |
65182-56-1
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| PubChem CID |
2761113
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| Appearance |
Yellow to orange solid powder
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| Melting Point |
92-94ºC
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| LogP |
3.002
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
259
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AYKMXKNVEUMLFQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H10N2O/c17-13-6-2-1-5-11(13)12-8-7-10-4-3-9-15-14(10)16-12/h1-9,17H
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| Chemical Name |
2-(1,8-naphthyridin-2-yl)phenol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~224.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4996 mL | 22.4982 mL | 44.9964 mL | |
| 5 mM | 0.8999 mL | 4.4996 mL | 8.9993 mL | |
| 10 mM | 0.4500 mL | 2.2498 mL | 4.4996 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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