534333 PI5P4Kγ Inhibitor, NIH-12848 - Calbiochem

534333
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₀H₁₄F₃N₃S

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      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.34333.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable quinazolinamine based compound that acts as a highly selective, non-ATP-competitive, and reversible inhibitor of phosphatidylinositol-5-phosphate-4-kinase γ (PI5P4Kγ; apparent IC50 ~ 3.3 µM), but does not inhibit the activity of PI5P4Kα and PI5P4Kβ even at higher concentration (~100 µM). Suggested to bind at the PI5P binding region, including the activation loop. Also shown to be effective against E378H, I159V, and D161V mutant forms of PI5P4Kγ (71% inhibition at 10 µM). However, N165I mutant enzyme is resistant to its action even at higher concentration (~50 µM). Blocks the translocation of Na+/K+-ATPase to the plasma membrane in confluent mouse principal kidney cortical collecting duct (mpkCCD) cells in culture and prevents dome formation.

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number534333
          Brand Family Calbiochem®
          SynonymsN-(Thiophen-2-ylmethyl)-2-(2-(trifluoromethyl)phenyl)quinazolin-4-amine, Phosphatidylinositol-5-phosphate-4-kinase γ Inhibitor, NCGC00012848-02
          DescriptionPI5P4Kγ Inhibitor, NIH-12848
          References
          ReferencesClarke, J.H., et al. 2015. Biochem. J.. 466, 359.
          Liang, Q., et al. 2014. Nat. Chem. Biol. 10, 298.
          Product Information
          FormWhite solid
          Hill FormulaC₂₀H₁₄F₃N₃S
          Chemical formulaC₂₀H₁₄F₃N₃S
          ReversibleY
          Quality LevelMQ100
          Applications
          Biological Information
          Primary TargetPI5P4Kγ
          Purity≥98% 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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          PI5P4Kγ Inhibitor, NIH-12848 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Clarke, J.H., et al. 2015. Biochem. J.. 466, 359.
          Liang, Q., et al. 2014. Nat. Chem. Biol. 10, 298.
          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.

          Revision25-June-2016 JSW
          SynonymsN-(Thiophen-2-ylmethyl)-2-(2-(trifluoromethyl)phenyl)quinazolin-4-amine, Phosphatidylinositol-5-phosphate-4-kinase γ Inhibitor, NCGC00012848-02
          DescriptionA cell-permeable quinazolinamine based compound that acts as a highly selective, non-ATP-competitive, and reversible inhibitor of phosphatidylinositol-5-phosphate-4-kinase γ (PI5P4Kγ; apparent IC50 ~ 3.3 µM), but does not inhibit the activity of PI5P4Kα and PI5P4Kβ even at higher concentration (~100 µM). Suggested to bind at the PI5P binding region, including the activation loop. Also shown to be effective against E378H, I159V, and D161V mutant forms of PI5P4Kγ (71% inhibition at 10 µM). However, N165I mutant enzyme is resistant to its action even at higher concentration (~50 µM). Blocks the translocation of Na+/K+-ATPase to the plasma membrane in confluent mouse principal kidney cortical collecting duct (mpkCCD) cells in culture and prevents dome formation.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₀H₁₄F₃N₃S
          Purity≥98% by HPLC
          SolubilityDMSO (50 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesClarke, J.H., et al. 2015. Biochem. J.. 466, 359.
          Liang, Q., et al. 2014. Nat. Chem. Biol. 10, 298.