NVP 231

Catalog No.S6501 Batch:S650101

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Technical Data

Formula

C25H25N3O2S
Molecular Weight 431.55 CAS No. 362003-83-6
Solubility (25°C)* In vitro DMSO 86 mg/mL (199.28 mM)
Ethanol 8 mg/mL (18.53 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

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 (from reference)

Cell Assay:

[2]
  • 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.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.