Biological Activity
Inhibitor of Ca2+-dependent Cl- channel (CaCC) transmembrane protein 16A (TMEM16A) (IC50 = 1.8 μM in A253 salivary gland epithelial cells). Inhibits EGF-induced increases in CaCC currents; blocks proliferation of tumor cells in vitro.
Technical Data
| M. Wt | 416.52 |
| Formula | C19H20N4O3S2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 552309-42-9 |
| PubChem ID | 3193184 |
| InChI Key | QSIYTNYMBWYHAA-UHFFFAOYSA-N |
| Smiles | CC1=NC(SCC(NC2=NC(C3=CC=C(OC)C=C3)=CS2)=O)=NC(O)=C1CC |
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 | 41.65 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 416.52. 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 | 24.01 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.
Namkung et al (2011) TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloride channel conductance in airway and intestinal epithelial cells. J.Biol.Chem. 286 2365 PMID: 21084298
Mroz and Keely (2012) Epidermal growth factor chronically upregulates Ca2+-dependent Cl- conductance and TMEM16A expression in intestinal epithelial cells. J.Physiol. 590 1907 PMID: 22351639
Duvvuri et al (2012) TMEM16A induces MAPK and contributes directly to tumorigenesis and cancer progression. Cancer Res. [Epub ahead of print] PMID: 22564524
Keywords: T16Ainh - A01, supplier, T16Ainh-A01, supplier, ca2+, calcium, activated, sensitive, chloride, Cl-, channels, CaCC, transmembrane, TMEM16A, inhibitors, inhibits, antiproliferative, antitumor, Ca2+-Activated, Chloride, Channels, Ca2+-Activated, Chloride, Channels, Tocris Bioscience
