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219493 Ceramide Kinase Inhibitor II, NVP-231 - Calbiochem

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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₅H₂₆N₃O₂S
Description
OverviewA cell-permeable benzothiazole compound that potently inhibits Cer (ceramide) phosphorylation by CerK (Cer Kinase) in a reversible and Cer-, but not ATP-, competitive manner (IC50 = 12 nM; Ki = 7.4 nM) with excellent selectivity over hDAGKα (IC50 = 5 µM) and little or no activity against eight other lipid metabolizing enzymes and kinases (IC50 ≥10 µM) in cell-free enzymatic assays. When applied to live cells in cultures, NVP-231 effectively prevents the binding of Cer to CerK, making cellular Cer more available to other Cer metabolizing enzymes and resulting in an increased GlcCer (glucosylceramide) and SM (sphingomyelin) production in addition to the expected decrease of Cer phosphorylation.
Catalogue Number219493
Brand Family Calbiochem®
SynonymsAdamantane-1-carboxylic acid-(2-benzoylamino-benzothiazol-6-yl)-amide, CerK Inhibitor II, NVP-231
References
ReferencesGraf, C., et al. 2008. Mol. Pharmacol. 74, 925.
Product Information
FormTan solid
Hill FormulaC₂₅H₂₆N₃O₂S
Chemical formulaC₂₅H₂₆N₃O₂S
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
219493 0

Documentation

Ceramide Kinase Inhibitor II, NVP-231 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Ceramide Kinase Inhibitor II, NVP-231 - Calbiochem Certificates of Analysis

TitleLot Number
219493

References

Reference overview
Graf, C., et al. 2008. Mol. Pharmacol. 74, 925.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision12-September-2011 RFH
SynonymsAdamantane-1-carboxylic acid-(2-benzoylamino-benzothiazol-6-yl)-amide, CerK Inhibitor II, NVP-231
DescriptionA cell-permeable benzothiazole compound that potently inhibits Cer (ceramide) phosphorylation by CerK (Cer Kinase) in a reversible and Cer-, but not ATP-, competitive manner (IC50 = 12 nM; Ki = 7.4 nM) with excellent selectivity over hDAGKα (IC50 = 5 µM) and little or no activity against eight other lipid metabolizing enzymes and kinases (IC50 ≥10 µM) in cell-free enzymatic assays. When applied to live cells in cultures, NVP-231 effectively prevents the binding of Cer to CerK, making cellular Cer more available to other Cer metabolizing enzymes and resulting in an increased GlcCer (glucosylceramide) and SM (sphingomyelin) production in addition to the expected decrease of Cer phosphorylation.
FormTan solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₅H₂₆N₃O₂S
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (25 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesGraf, C., et al. 2008. Mol. Pharmacol. 74, 925.