Description: Potent and selective PDE4 inhibitor; suppresses hedgehog signaling
Chemical Name: 5,6,7,8-Tetrahydro-3-(2-methyl-2-propen-1-yl)-2-[[2-oxo-2-(2-thienyl)ethyl]thio]-[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent and selective phosphodiesterase (PDE) 4 inhibitor (IC50 = 72 nM). Exhibits >40-fold selectivity over PDE3, PDE10, and PDE11. Displays no significant activity on a panel of 442 kinases, 158 GPCRs and 21 phosphatases. Suppresses hedgehog signaling through PDE antagonism, downstream of smoothened signaling. Reduces transcription of Gli1 and Ptc1.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
8.33
20
Preparing Stock Solutions
The following data is based on the product molecular weight 416.58. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.4 mL
12 mL
24 mL
5 mM
0.48 mL
2.4 mL
4.8 mL
10 mM
0.24 mL
1.2 mL
2.4 mL
50 mM
0.05 mL
0.24 mL
0.48 mL
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
Select another language:
View SDS
References
References are publications that support the products' biological activity.
Williamset al (2015) An in vivo chemical genetic screen identifies phosphodiesterase 4 as a pharmacological target for hedgehog signaling inhibition. Cell Rep. 11 43 PMID: 25818300