NVP 231

For research use only.

Catalog No.S6501

NVP 231 Chemical Structure

CAS No. 362003-83-6

NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 12 nM. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage.

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Description NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 12 nM. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage.
Targets
CreK [1]
(Cell-free assay)
12 nM
In vitro

NVP-231 reduces cell viability and DNA synthesis by triggering cell death of cancer cells. NVP-231-treated cells committed M phase arrest rather than arrest at the G2/M boundary. In MCF-7 and NCI-H358 cells, NVP-231 treatment causes a concentration-dependent up-regulation of cyclin B1 phosphorylation at Ser133 and a reduction of CDK1 phosphorylation at Tyr15. Wee1 is down-regulated by NVP-231 in both NCI-H358 and MCF-7 cells. Upon NVP-231 treatment of cancer cells, CDK4 protein is concentration- and time-dependently down-regulated. This effect is even more pronounced in synchronized cells[2].

Protocol

Cell Research:

[2]

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  • Cell lines: MCF-7 and NCI H358 cells
  • Concentrations: 10, 100, 300, 500 and 1000 nM
  • Incubation Time: 4 h
  • Method:

    MCF-7 and NCI-H358 cells are plated in a 96-well black plate (1 × 104 cells per well) and treated for 48 h with either vehicle (Co) or the indicated concentrations of NVP-231 (in nM). For the last 4 h of treatment, alamarBlueR is added and fluorescence is determined.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (199.28 mM)
Ethanol 8 mg/mL (18.53 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 431.55
Formula

C25H25N3O2S

CAS No. 362003-83-6
Storage powder
in solvent
Synonyms N/A
Smiles C1C2CC3CC1CC(C2)(C3)C(=O)NC4=CC5=C(C=C4)N=C(S5)NC(=O)C6=CC=CC=C6

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID