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

406170
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₀H₁₆F₃N₇O₂ 519178-28-0

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      406170-5MG
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          Plastic ampoule 5 mg
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          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®
          SynonymsInositol-1,4,5-trisphosphate 3-Kinase Inhibitor, N²-(m-Trifluorobenzyl), N⁶-(p-nitrobenzyl)purine, 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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          406170

          References

          Reference overview
          Padmanabhan, U., et al. 2009. J. Biol. Chem. 284, 10571. Chang, Y.T., et al. 2002. ChemBioChem 3, 897.

          Brochure

          Title
          Calbiochem Biologics 32.2
          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.

          Revision23-February-2011 JSW
          SynonymsInositol-1,4,5-trisphosphate 3-Kinase Inhibitor, N²-(m-Trifluorobenzyl), N⁶-(p-nitrobenzyl)purine, 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.