Biochem/physiol Actions

Reversible: yes

Target IC₅₀: 72 nM for PDE4D3

Primary TargetPDE4D3

Cell permeable: yes

General description

A cell-permeable thienopyrimidinone compound that acts as a potent and reversible inhibitor of phosphodiesterase IV (IC₅₀ = 72 nM for PDE4D3). Inhibits other PDEs at 40-50-fold higher concentrations (IC₅₀ = 3.00, 3.05 and 4.08 µM for PDE3A, PDE10A2 and PDE11A4, respectively). Displays excellent selectivity over a wide panel of kinases, GPCRs and phosphatases at 10 µM. Shown to robustly activate PKA and block Hedgehog (Hh) signaling downstream of Smoothened. Significantly reduces Gli1 and Ptc1 transcription levels in MEFs and efficiently induces Hh-null phenotype in zebrafish at 2 µM.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.

A cell-permeable thienopyrimidinone compound that acts as a potent and reversible inhibitor of phosphodiesterase IV (IC₅₀ = 72 nM for PDE4D3). Inhibits other PDEs at 40-50-fold higher concentrations (IC₅₀ = 3.00, 3.05 and 4.08 µM for PDE3A, PDE10A2 and PDE11A4, respectively). Displays excellent selectivity over a wide panel of kinases, GPCRs and phosphatases at 10 µM. Shown to robustly activate PKA and block Hedgehog (Hh) signaling downstream of Smoothened. Significantly reduces Gli1 and Ptc1 transcription levels in MEFs and efficiently induces Hh-null phenotype in zebrafish at 2 µM.

Legal Information

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

Other Notes

Williams, C.H., et al. 2015. Cell Reports.11, 43.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)