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5.34333 Sigma-Aldrich

PI5P4Kγ Inhibitor, NIH-12848 - Calbiochem

Synonym: N-(Thiophen-2-ylmethyl)-2-(2-(trifluoromethyl)phenyl)quinazolin-4-amine, Phosphatidylinositol-5-phosphate-4-kinase γ Inhibitor, NCGC00012848-02, PI5P4Kγ Inhibitor, NIH-12848 - Calbiochem

  • Empirical Formula (Hill Notation) C20H14F3N3S

  • Molecular Weight 385.41

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Properties

Quality Level   100
assay   ≥98% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   white
solubility   DMSO: 50 mg/mL

Description

General description

A 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.

A 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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PI5P4Kγ

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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