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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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: PI5P4Kγ
534333
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
959551-10-1C₂₀H₁₄F₃N₃S

Products

Catalogue NumberPackaging Qty/Pack
5343330001 Glass bottle 10 mg
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
Catalogue Number GTIN
5343330001 04054839059377

Documentation

PI5P4Kγ Inhibitor, NIH-12848 - CAS 959551-10-1 - 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
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.