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406170 IP6K Inhibitor - CAS 519178-28-0 - Calbiochem

406170
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Panoramica

Replacement Information

Tabella delle specifiche principali

Empirical FormulaCAS #
C₂₀H₁₆F₃N₇O₂ 519178-28-0

Products

Numero di catalogoConfezionamento Qtà/conf
406170-5MG Fiala di plastica 5 mg
Description
OverviewA cell-permeable 2,6-disubstituted purine compound that, although originally identified as a reversible, ATP-competitive inhibitor against the conversion of Ins(1,4,5)P3 (Cat. Nos. 407123 & 407137) to Ins(1,3,4,5)P4 (Cat. No. 407126) by IP3K (IC50 = 18 µM; [ATP] = 10 μM), acts in fact as a much more effective inhibitor against the IP6K1/2/3-catalyzed conversion of InsP6 (Cat. No. 407125) to 5-[PP]- InsP6 or InsP7 (IC50 = 0.47 μM against IP6K1; [ATP] = 1 mM) due to a much higher affinity of ATP toward IP3K than IP6K (Km of ATP for the respective enzymes = 0.01 vs 1000 μM). Shown to potently inhibit cellular InsP7 level (IC50 = 0.55 μM in HeLa cultures), while being less potent in increasing the cellular InsP3 accumulation (>10 µM in HeLa cultures). TNP is also effective against S. cerevisiae IP6K, Kcs1, but not Vip/PPIP5Ks, enzymes that catalyze the pyrophosphorylation at the 1/3 position of InsP6 and InsP7, in either human or yeast species or two other IP3 metabolizing enzymes, PLC and IP3 5-ppase.
Catalogue Number406170
Brand Family Calbiochem®
SynonymsN²-(m-Trifluorobenzyl), N⁶-(p-nitrobenzyl)purine, Inositol-1,4,5-trisphosphate 3-Kinase Inhibitor, IP3K Inhibitor, Kcs1 Inhibitor, TNP
References
ReferencesPadmanabhan, U., et al. 2009. J. Biol. Chem. 284, 10571. Chang, Y.T., et al. 2002. ChemBioChem 3, 897.
Product Information
CAS number519178-28-0
ATP CompetitiveY
FormYellow solid
Hill FormulaC₂₀H₁₆F₃N₇O₂
Chemical formulaC₂₀H₁₆F₃N₇O₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetIP 3-K
Primary Target IC<sub>50</sub>0.47 µM against IP6K1; [ATP] = 1 mM; 18 µM against the conversion of Ins(1,4,5)P3 to Ins(1,3,4,5)P4 by IP3K; [ATP] = 10 µM
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
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

Documentation

IP6K Inhibitor - CAS 519178-28-0 - Calbiochem MSDS

Titolo

Scheda di sicurezza (MSDS) 

IP6K Inhibitor - CAS 519178-28-0 - Calbiochem Certificati d'Analisi

TitoloNumero di lotto
406170

Riferimenti bibliografici

Panoramica delle referenze
Padmanabhan, U., et al. 2009. J. Biol. Chem. 284, 10571. Chang, Y.T., et al. 2002. ChemBioChem 3, 897.
Scheda tecnica

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.

Revision23-February-2011 JSW
SynonymsN²-(m-Trifluorobenzyl), N⁶-(p-nitrobenzyl)purine, Inositol-1,4,5-trisphosphate 3-Kinase Inhibitor, IP3K Inhibitor, Kcs1 Inhibitor, TNP
DescriptionA cell-permeable 2,6-disubstituted purine compound that, although originally identified as a reversible, ATP-competitive inhibitor against the conversion of Ins(1,4,5)P3 (Cat. Nos. 407123 & 407137) to Ins(1,3,4,5)P4 (Cat. No. 407126) by IP3K (IC50 = 18 µM; [ATP] = 10 μM), acts in fact as a much more effective inhibitor against the IP6K1/2/3-catalyzed conversion of InsP6 (Cat. No. 407125) to 5-[PP]- InsP6 or InsP7 (IC50 = 0.47 μM against IP6K1; [ATP] = 1 mM) due to a much higher affinity of ATP toward IP3K than IP6K (Km of ATP for the respective enzymes = 0.01 vs 1000 μM). Shown to potently inhibit cellular InsP7 level (IC50 = 0.55 μM in HeLa cultures), while being less potent in increasing the cellular InsP3 accumulation (>10 µM in HeLa cultures). TNP is also effective against S. cerevisiae IP6K, Kcs1, but not Vip/PPIP5Ks, enzymes that catalyze the pyrophosphorylation at the 1/3 position of InsP6 and InsP7, in either human or yeast species or two other IP3 metabolizing enzymes, PLC and IP3 5-ppase.
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number519178-28-0
Chemical formulaC₂₀H₁₆F₃N₇O₂
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (10 mg/ml) or Methanol (5 mg/ml)
Storage +2°C to +8°C
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.
Toxicity Standard Handling
ReferencesPadmanabhan, U., et al. 2009. J. Biol. Chem. 284, 10571. Chang, Y.T., et al. 2002. ChemBioChem 3, 897.