Home >> Research Area >>Others>>CERK>> NVP 231

NVP 231

CerK inhibitor CAS# 362003-83-6

NVP 231

Catalog No. BCC4244----Order now to get a substantial discount!

Product Name & Size Price Stock
NVP 231: 5mg $23 In Stock
NVP 231: 10mg Please Inquire In Stock
NVP 231: 20mg Please Inquire Please Inquire
NVP 231: 50mg Please Inquire Please Inquire
NVP 231: 100mg Please Inquire Please Inquire
NVP 231: 200mg Please Inquire Please Inquire
NVP 231: 500mg Please Inquire Please Inquire
NVP 231: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of NVP 231

Number of papers citing our products

Chemical structure

NVP 231

3D structure

Chemical Properties of NVP 231

Cas No. 362003-83-6 SDF Download SDF
PubChem ID 4096211 Appearance Powder
Formula C25H25N3O2S M.Wt 431.55
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 5 mM in ethanol
Chemical Name N-(2-benzamido-1,3-benzothiazol-6-yl)adamantane-1-carboxamide
SMILES C1C2CC3CC1CC(C2)(C3)C(=O)NC4=CC5=C(C=C4)N=C(S5)NC(=O)C6=CC=CC=C6
Standard InChIKey MVSSJPGNLQPWSW-UHFFFAOYSA-N
Standard InChI InChI=1S/C25H25N3O2S/c29-22(18-4-2-1-3-5-18)28-24-27-20-7-6-19(11-21(20)31-24)26-23(30)25-12-15-8-16(13-25)10-17(9-15)14-25/h1-7,11,15-17H,8-10,12-14H2,(H,26,30)(H,27,28,29)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of NVP 231

DescriptionPotent, selective and reversible ceramide kinase (CerK) inhibitor (IC50 = 12 nM in vitro). Displays selectivity for CerK over sphingosine kinases (IC50 ≥100 μM) and other lipid kinases.

NVP 231 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

NVP 231 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of NVP 231

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3172 mL 11.5861 mL 23.1723 mL 46.3446 mL 57.9307 mL
5 mM 0.4634 mL 2.3172 mL 4.6345 mL 9.2689 mL 11.5861 mL
10 mM 0.2317 mL 1.1586 mL 2.3172 mL 4.6345 mL 5.7931 mL
50 mM 0.0463 mL 0.2317 mL 0.4634 mL 0.9269 mL 1.1586 mL
100 mM 0.0232 mL 0.1159 mL 0.2317 mL 0.4634 mL 0.5793 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on NVP 231

NVP 231 is a potent, reversible and specific inhibitor of ceramide kinase(CerK) with the IC50 value of 12±2nM in radio assay [1].

NVP 231 has been noted to inhibit CerK with the IC50 value of 12±2nM and have the 90% inhibition at 100 nM in the radio assay. In addition, NVP 231 has been reported to compete with ceramide with the Ki value of 7.4 nM. Furthermore, NVP 231 has been revealed to achieve complete inhibition of CIP at 100nM. NVP 231 in an assay based on human CerK-overexpressing COS-cells (COS-CerK). And the study has been exhibited that NVP 231 is a more potent inhibitor of mouse CerK. Apart from these, NVP 231 has been shown the specificity to CerK with the IC50 values of 0.01 μM, 100 μM, >100 μM, 5 μM, >25 μM, >25 μM, >10 μM, >10 μM and >10 μM for hCerK, hSphK1, hSphK2, hDAGKα, hPI3Kα, hVps34, hGCS, hSMS-1 and CERT, respectively [1].

References:
[1]Graf C1, Klumpp M, Habig M, Rovina P, Billich A, Baumruker T, Oberhauser B, Bornancin F. Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor. Mol Pharmacol. 2008 Oct;74(4):925-32.

,

Featured Products
New Products
 

References on NVP 231

The ceramide kinase inhibitor NVP-231 inhibits breast and lung cancer cell proliferation by inducing M phase arrest and subsequent cell death.[Pubmed:25134723]

Br J Pharmacol. 2014 Dec;171(24):5829-44.

BACKGROUND AND PURPOSE: Ceramide kinase (CerK) catalyzes the generation of ceramide-1-phosphate which may regulate various cellular functions, including inflammatory reactions and cell growth. Here, we studied the effect of a recently developed CerK inhibitor, NVP-231, on cancer cell proliferation and viability and investigated the role of cell cycle regulators implicated in these responses. EXPERIMENTAL APPROACH: The breast and lung cancer cell lines MCF-7 and NCI-H358 were treated with increasing concentrations of NVP-231 and DNA synthesis, colony formation and cell death were determined. Flow cytometry was performed to analyse cell cycle distribution of cells and Western blot analysis was used to detect changes in cell cycle regulator expression and activation. KEY RESULTS: In both cell lines, NVP-231 concentration-dependently reduced cell viability, DNA synthesis and colony formation. Moreover it induced apoptosis, as measured by increased DNA fragmentation and caspase-3 and caspase-9 cleavage. Cell cycle analysis revealed that NVP-231 decreased the number of cells in S phase and induced M phase arrest with an increased mitotic index, as determined by increased histone H3 phosphorylation. The effect on the cell cycle was even more pronounced when NVP-231 treatment was combined with staurosporine. Finally, overexpression of CerK protected, whereas down-regulation of CerK with siRNA sensitized, cells for staurosporine-induced apoptosis. CONCLUSIONS AND IMPLICATIONS: Our data demonstrate for the first time a crucial role for CerK in the M phase control in cancer cells and suggest its targeted inhibition, using drugs such as NVP-231, in combination with conventional pro-apoptotic chemotherapy.

A secondary assay for ceramide kinase inhibitors based on cell growth inhibition by short-chain ceramides.[Pubmed:18831956]

Anal Biochem. 2009 Jan 1;384(1):166-9.

We recently reported that ectopic expression of ceramide kinase (CerK) in various cell lines increases their sensitivity to cell death induced by the exogenous addition of short-chain (e.g., C2) ceramides (Cer). Here we show that this higher sensitivity results from CerK catalytic activity and production of C2-ceramide 1-phosphate (C2-C1P). If CerK activity is inhibited by the potent inhibitor NVP-231, C2-C1P is not produced and viability returns to control levels. The EC(50) of NVP-231 in this assay is in the low nanomolar range, consistent with the IC(50) determined in activity assays in vitro using purified CerK. NVP-995, a structurally related but inactive compound, does not protect against C2-Cer-induced cell death. This assay is robust and easy to implement and scale up, thereby providing a valuable secondary screen assay for CerK inhibitors.

Ceramide kinase deficiency impairs microendothelial cell angiogenesis in vitro.[Pubmed:19323974]

Microvasc Res. 2009 May;77(3):389-93.

The recent generation of ceramide kinase (CerK)-deficient (Cerk (-/-)) mice as well as the identification of the potent CerK inhibitor NVP-231 have provided unprecedented opportunities to better understand CerK biology. Here we used skin dermal microendothelial cells (DMECs) and we show that CerK activity regulates their neovascularization in a matrigel environment in vitro. Capillary-like tube formation was significantly impaired in CerK-deficient cells or in wild-type (WT) cells treated with NVP-231 as compared with untreated WT cells. This was not the result of compromised proliferation or survival because Cerk (-/-) endothelial cells were able to migrate out of dermal fragments and grow in monolayer culture as well as their WT counterpart. Vascular endothelial growth factor, fibroblast growth factor or tumor necrosis factor could not rescue the angiogenesis defect observed in Cerk (-/-) DMEMs. Moreover, CerK ablation increased serum ceramide levels at the expense of dihydroceramide levels without affecting sphingosine, dihydrosphingosine, sphingosine-1-phosphate or dihydrosphingosine-1-phosphate levels. These observations collectively suggest that CerK-catalyzed formation of C1P may regulate angiogenesis by a novel mechanism that is independent of S1P formation and signaling.

Description

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.

Keywords:

NVP 231,362003-83-6,Natural Products,CERK, buy NVP 231 , NVP 231 supplier , purchase NVP 231 , NVP 231 cost , NVP 231 manufacturer , order NVP 231 , high purity NVP 231

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: