2. Apoptosis
  3. Apoptosis
  4. NVP 231

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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NVP 231 Chemical Structure

NVP 231 Chemical Structure

CAS No. : 362003-83-6

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Based on 2 publication(s) in Google Scholar

NVP 231 Related Antibodies

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Description

NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK[1]. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage[2].

IC50 & Target

IC50: 12 nM (CerK); apoptosis[1][3]
In Vitro

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.

NVP 231 Related Antibodies

Cell Viability Assay[3]

Cell Line: MCF-7 cells; NCI-H358 cells
Concentration: 0 nM, 10 nM, 100 nM, 300 nM, 500 nM, 1000 nM
Incubation Time: 48 hours
Result: Reduced MCF-7 cells and NCI-H358 cells in a concentration manner.

Apoptosis Analysis[3]

Cell Line: MCF-7 cells; NCI-H358 cells
Concentration: 1000 nM
Incubation Time: 24-72 hours
Result: Increases caspase-3 and caspase-9 cleavage in MCF-7 and NCI-H358 cells.

Western Blot Analysis[3]

Cell Line: MCF-7 cells; NCI-H358 cells
Concentration: 0 nM, 100 nM, 300 nM, 500 nM
Incubation Time: 24 hours
Result: Decreased p-cyclin B1, p-CDK1 as a concentration manner.
Molecular Weight

431.55

Formula

C25H25N3O2S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3172 mL 11.5861 mL 23.1723 mL
5 mM 0.4634 mL 2.3172 mL 4.6345 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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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NVP 231 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NVP 231362003-83-6NVP231NVP-231Apoptosisapoptosiscancermcf-7 NCI-H358cerkInhibitorinhibitorinhibit

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