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.
Technical Data
| M. Wt | 416.58 |
| Formula | C20H20N2O2S3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 505068-32-6 |
| PubChem ID | 1158635 |
| InChI Key | XAKJIQPEGSCYIP-UHFFFAOYSA-N |
| Smiles | CC(CN1C(C2=C(N=C1SCC(C3=CC=CS3)=O)SC4=C2CCCC4)=O)=C |
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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
Williams et 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
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