Biochem/physiol Actions

Primary TargetPI5P4Kγ

Reversible: yes

Cell permeable: yes

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 PI5P4KA 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 PI5P4KA 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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)