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534333 PI5P4Kγ Inhibitor, NIH-12848 - CAS 959551-10-1 - Calbiochem

A cell-permeable, selective, non-ATP-competitive, reversible inhibitor of PI5P4Kg (IC₅₀ ~ 3.3 µM). Does not inhibit the activity of PI5P4Ka and b even at higher concentration (~100 µM).

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Synonyme: N-(Thiophen-2-ylmethyl)-2-(2-(trifluoromethyl)phenyl)quinazolin-4-amine, Phosphatidylinositol-5-phosphate-4-kinase γ Inhibitor, NCGC00012848-02

Primary Target: PI5P4Kγ
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534333
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
959551-10-1C₂₀H₁₄F₃N₃S

Preis & Verfügbarkeit

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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
      CAS number959551-10-1
      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
      Global Trade Item Number
      Bestellnummer GTIN
      5.34333.0001 04054839059377

      Documentation

      PI5P4Kγ Inhibitor, NIH-12848 - CAS 959551-10-1 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

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

      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
      CAS number959551-10-1
      Chemical formulaC₂₀H₁₄F₃N₃S
      Purity≥98% by HPLC
      SolubilityDMSO (50 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 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.