NVP 231
Based on 3 publication(s) in Google Scholar
NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage.
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- Reinheit: 99.73%
- CAS. Nr.: 362003-83-6
- Formel: C25H25N3O2S
- Molecular Weight:431.55
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) NVP 231
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Biologische Aktivität
NVP-231 (0-500 nM; 24 hours) gradually reduces the cellular CerK activity, as measured by NBD-C1P formation, demonstrating that NVP-231 active in transfected cells. The IC50 for CerK in this cellular system is 59.70 ± 12 nM[3]. NVP-231 (0-1000 nM; 48 hours) decreases cell viability as a dose-dependent manner. This compound shows IC50 values of 1 μM in MCF-7 cells and 500 nM in NCI-H358 cells[3]. NVP-231 (1 μM; 24-72 hours) induces caspase-3 and caspase-9 cleavage in both cell lines. However, the highest caspase-3 and caspase-9 cleavage and activation occurred at 24 hours in MCF-7 cells, then decreases again. In NCI-H358 cells, caspase-3 and caspase-9 cleavage occurrs continuously over 72 hours[3]. NVP-231 (0-500 nM; 24 hours) causes a concentration-dependent up-regulation of cyclin B1 phosphorylation at Ser133 and a reduction of CDK1 phosphorylation at Tyr15. The total CDK1 expression also declined upon CerK inhibition[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells; NCI-H358 cells
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Concentration:0 nM, 10 nM, 100 nM, 300 nM, 500 nM, 1000 nM
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Incubation Time:48 hours
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Result:Reduced MCF-7 cells and NCI-H358 cells in a concentration manner.
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Cell Line:MCF-7 cells; NCI-H358 cells
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Concentration:1000 nM
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Incubation Time:24-72 hours
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Result:Increases caspase-3 and caspase-9 cleavage in MCF-7 and NCI-H358 cells.
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Cell Line:MCF-7 cells; NCI-H358 cells
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Concentration:0 nM, 100 nM, 300 nM, 500 nM
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Incubation Time:24 hours
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Result:Decreased p-cyclin B1, p-CDK1 as a concentration manner.
Chemical Information
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CAS. Nr. 362003-83-6
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Appearance Solid
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Molecular Weight 431.55
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Formel C25H25N3O2S
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Color White to off-white
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SMILES
O=C(C1(C[C@@H](C2)C3)C[C@@H]3C[C@@H]2C1)NC4=CC=C5N=C(NC(C6=CC=CC=C6)=O)SC5=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Pharmacol Res
Ceramide kinase confers tamoxifen resistance in estrogen receptor-positive breast cancer by altering sphingolipid metabolism. [Abstract]2023 Jan:187:106558. PMID: 36410675 -
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bioRxiv
Multiplexed single-cell lineage tracing of mitotic kinesin inhibitor resistance in glioblastoma. [Abstract]2023 Sep 12:2023.09.09.557001. PMID: 37745469
Lösungsmittel & Löslichkeit
DMSO : ≥ 41 mg/mL (95.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Graf C, et al. Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor. Mol Pharmacol. 2008 Oct;74(4):925-32. [Content Brief]
[2]. Graf C, et al. A secondary assay for ceramide kinase inhibitors based on cell growth inhibition by short-chain ceramides. Anal Biochem. 2009 Jan 1;384(1):166-9. [Content Brief]
[3]. Pastukhov O,et al. The ceramide kinase inhibitor NVP-231 inhibits breast and lung cancer cell proliferation by inducing M phase arrest and subsequent cell death.Br J Pharmacol. 2014 Dec;171(24):5829-44. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3172 mL | 11.5861 mL | 23.1723 mL | 57.9307 mL |
| 5 mM | 0.4634 mL | 2.3172 mL | 4.6345 mL | 11.5861 mL | |
| 10 mM | 0.2317 mL | 1.1586 mL | 2.3172 mL | 5.7931 mL | |
| 15 mM | 0.1545 mL | 0.7724 mL | 1.5448 mL | 3.8620 mL | |
| 20 mM | 0.1159 mL | 0.5793 mL | 1.1586 mL | 2.8965 mL | |
| 25 mM | 0.0927 mL | 0.4634 mL | 0.9269 mL | 2.3172 mL | |
| 30 mM | 0.0772 mL | 0.3862 mL | 0.7724 mL | 1.9310 mL | |
| 40 mM | 0.0579 mL | 0.2897 mL | 0.5793 mL | 1.4483 mL | |
| 50 mM | 0.0463 mL | 0.2317 mL | 0.4634 mL | 1.1586 mL | |
| 60 mM | 0.0386 mL | 0.1931 mL | 0.3862 mL | 0.9655 mL | |
| 80 mM | 0.0290 mL | 0.1448 mL | 0.2897 mL | 0.7241 mL |
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