Home Apoptosis Caspase activator - Other inhibitor NVP 231 For research use only.

NVP 231

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.

NVP 231 Chemical Structure

NVP 231 Chemical Structure

CAS: 362003-83-6

Purity & Quality Control

Batch: Purity: 99.30%
99.30

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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
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].
Cell Research 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.

Chemical Information & Solubility

Molecular Weight 431.55 Formula

C25H25N3O2S
CAS No. 362003-83-6 SDF --
Smiles C1C2CC3CC1CC(C2)(C3)C(=O)NC4=CC5=C(C=C4)N=C(S5)NC(=O)C6=CC=CC=C6
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 86 mg/mL ( (199.28 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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