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  3. NVP 231

NVP 231 

Cat. No.: HY-13945 Purity: 98.91%
Handling Instructions

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.

For research use only. We do not sell to patients.

NVP 231 Chemical Structure

NVP 231 Chemical Structure

CAS No. : 362003-83-6

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Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 61 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 55 In-stock
Estimated Time of Arrival: December 31
50 mg USD 150 In-stock
Estimated Time of Arrival: December 31
100 mg USD 250 In-stock
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500 mg USD 950 In-stock
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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 41 mg/mL (95.01 mM)

*"≥" 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
10 mM 0.2317 mL 1.1586 mL 2.3172 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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NVP 231
Cat. No.:
HY-13945
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