NV914
Based on 1 Customer Validation
NV914 is an inhibitor of FTSJ1 (tryptophan tRNA-specific 2'-O-methyltransferase) that inhibits the methyltransferase activity of FTSJ1, induces translational readthrough of premature termination codons, and enables genes carrying nonsense mutations to synthesize full-length proteins. NV914 belongs to translational readthrough-inducing compounds (TRIDs). NV914 exhibits translational readthrough activity against nonsense mutations in in vitro systems, does not induce readthrough of natural termination codons, and restores CFTR protein expression. NV914 shows favorable acute oral tolerance in mice, with low health risks and good safety profiles. NV914 is applicable to research related to cystic fibrosis and Shwachman-Diamond syndrome.
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- Pureza: 98.98%
- No. CAS: 2341941-41-9
- Fòrmula: C15HF10N3O2
- Peso molecular:445.18
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
NV914 (3-48 μM; 24 h) does not induce NTC readthrough in HCT116 cells, as no higher molecular weight p53 bands are detected after treatment plus Doxorubicin[1].
NV914 (3-48 μM; 24 h) does not alter p53 nuclear localization in HCT116 cells after treatment plus Doxorubicin[1].
NV914 (3-48 μM; 24 h) does not impair p53 functionality (as measured by p21 mRNA expression) in HCT116 cells after treatment plus Doxorubicin[1].
NV914 (12-100 μM; 24 or 72 h) does not induce NTC readthrough in 16HBE cells, as no higher molecular weight Cys-C or β2M bands are detected after treatment[1].
NV914 (6-24 μM; 24 h) induces readthrough of the UGA premature termination codon in pFLuc190UGA-transfected HeLa cells, and this activity is counteracted by FTSJ1 overexpression[3].
NV914 (12 μM; 24 h) induces readthrough of the W1282X UGA premature termination codon in IB3.1 cystic fibrosis cells, and this activity is reduced by FTSJ1 overexpression[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 colon cancer cells
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Concentration:3-48 μM
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Incubation Time:24 h
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Result:Detected a slight decrease in p53 protein levels in cells treated with NV914 and Doxorubicin compared to Doxorubicin-only samples; showed no p53 bands with higher molecular weights (indicative of natural termination codon [NTC] readthrough).
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Cell Line:HCT116 colon cancer cells
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Concentration:3-48 μM
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Incubation Time:24 h
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Result:Localized p53 fluorescent signal in the cell nuclei in all cell samples treated with Doxorubicin and NV914; observed no significant change in p53 nuclear localization.
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Cell Line:16HBE human bronchial epithelial cells
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Concentration:12-100 μM (24 h treatment); 12-100 μM (72 h treatment, refreshed every 24 h)
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Incubation Time:24 h; 72 h (treatments refreshed every 24 h)
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Result:Detected no bands corresponding to higher molecular weight forms of Cys-C or β2M in cells treated with NV914 for 24 or 72 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (both sexes, 6-8 weeks old, weight 18±4 g)[2]
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Dosage:2000 mg/kg
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Administration:p.o.; single dose
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Result:Observed no mortality within 14 days.
Recorded hypoactivity in 5 of 6 treated mice, hyperactivity and abdominal pain in 4 of 6, tremors and convulsions in 3 of 6, itching and scratching in 2 of 6; resolved all toxicity signs within 3 h post-treatment.
Detected no significant difference in body weight growth patterns compared to controls.
Found no significant morphological alterations in analyzed organs, except for a slight tendency to maturation disturbance of neutrophil granulocytes and weak expansion of erythroid lineage in two bone marrow samples.
Chemical Information
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No. CAS 2341941-41-9
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Appearance Solid
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Peso molecular 445.18
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Fòrmula C15HF10N3O2
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Color White to off-white
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SMILES
O=C(NC1=NOC(=N1)C=2C(F)=C(F)C(F)=C(F)C2F)C=3C(F)=C(F)C(F)=C(F)C3F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (224.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Perriera R, et al. Readthrough Approach Using NV Translational Readthrough-Inducing Drugs (TRIDs): A Study of the Possible Off-Target Effects on Natural Termination Codons (NTCs) on TP53 and Housekeeping Gene Expression. Int J Mol Sci. 2023;24(20):15084. Published 2023 Oct 11. [Content Brief]
[2]. Corrao F, et al. Nonsense codons suppression. An acute toxicity study of three optimized TRIDs in murine model, safety and tolerability evaluation. Biomed Pharmacother. 2022;156:113886. [Content Brief]
[3]. Carollo PS, et al. Investigating the Inhibition of FTSJ1, a Tryptophan tRNA-Specific 2'-O-Methyltransferase by NV TRIDs, as a Mechanism of Readthrough in Nonsense Mutated CFTR. Int J Mol Sci. 2023;24(11):9609. Published 2023 Jun 1. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2463 mL | 11.2314 mL | 22.4628 mL | 56.1571 mL |
| 5 mM | 0.4493 mL | 2.2463 mL | 4.4926 mL | 11.2314 mL | |
| 10 mM | 0.2246 mL | 1.1231 mL | 2.2463 mL | 5.6157 mL | |
| 15 mM | 0.1498 mL | 0.7488 mL | 1.4975 mL | 3.7438 mL | |
| 20 mM | 0.1123 mL | 0.5616 mL | 1.1231 mL | 2.8079 mL | |
| 25 mM | 0.0899 mL | 0.4493 mL | 0.8985 mL | 2.2463 mL | |
| 30 mM | 0.0749 mL | 0.3744 mL | 0.7488 mL | 1.8719 mL | |
| 40 mM | 0.0562 mL | 0.2808 mL | 0.5616 mL | 1.4039 mL | |
| 50 mM | 0.0449 mL | 0.2246 mL | 0.4493 mL | 1.1231 mL | |
| 60 mM | 0.0374 mL | 0.1872 mL | 0.3744 mL | 0.9360 mL | |
| 80 mM | 0.0281 mL | 0.1404 mL | 0.2808 mL | 0.7020 mL | |
| 100 mM | 0.0225 mL | 0.1123 mL | 0.2246 mL | 0.5616 mL |
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