T16Ainh - A01

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Cat.No. 4538 - T16Ainh - A01 | C19H20N4O3S2 | CAS No. 552309-42-9
Description: Ca2+-activated Cl- channel transmembrane protein 16A (TMEM16A) inhibitor
Chemical Name: 2-[(5-Ethyl-1,6-dihydro-4-methyl-6-oxo-2-pyrimidinyl)thio]-N-[4-(4-methoxyphenyl)-2-thiazolyl]acetamide
Purity: ≥98% (HPLC)
Datasheet
Citations (7)
Reviews
Literature
Pathways

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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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References

References are publications that support the biological activity of the product.

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


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7 Citations for T16Ainh - A01

Citations are publications that use Tocris products. Selected citations for T16Ainh - A01 include:

Jeon et al (2013) Presynaptic Localization and Possible Function of Calcium-Activated Chloride Channel Anoctamin 1 in the Mammalian Retina. PLoS One 8 e67989 PMID: 23840801

Bijos et al (2014) Anoctamin-1 in the juvenile rat urinary bladder. PLoS One 9 e106190 PMID: 25181534

Bill et al (2014) Small molecule-facilitated degradation of ANO1 protein: a new targeting approach for anticancer therapeutics. J Biol Chem 289 11029 PMID: 24599954

Zhang et al (2015) Anoctamin Calcium-Activated Chloride Channels May Modulate Inhibitory Transmission in the Cerebellar Cortex. PLoS One 10 e0142160 PMID: 26558388

Harper and Poole (2013) Chloride channels are necessary for full platelet phosphatidylserine exposure and procoagulant activity. PLoS One 4 e969 PMID: 24357800

Zhang et al (2015) TMEM16A-Mediated Mucin Secretion in IL-13-Induced Nasal Epithelial Cells From Chronic Rhinosinusitis Patients. Mol Pain 7 367 PMID: 25749771

Pineda-Farias et al (2015) Role of anoctamin-1 and bestrophin-1 in spinal nerve ligation-induced neuropathic pain in rats. Cell Death Dis 11 41 PMID: 26130088


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