356102-14-2

Ani 9 is an inhibitor of the calcium-activated chloride channel (CaCC) anoctamin 1 (ANO1) that blocks ATP-induced apical membrane chloride currents in ANO1-expressing Fischer rat thyroid (FRT) cells (IC₅₀ = 77 nM). It is selective for ANO1 over ANO2 at 10 μM and the cystic fibrosis transmembrane conductance regulator (CFTR) and epithelial sodium channel (ENaC) at 30 μM. Ani 9 inhibits ATP-induced quenching of a fluorescent intracellular halide sensor in PC3 prostate cancer cells and Capan-1 pancreatic carcinoma cells in a concentration-dependent manner.

(4-Chloro-2-methylphenoxy)-[(2-methoxyphenyl)methylene]hydrazide Acetic Acid inhibits anoctamin1/transmembrane protein 16A, a calcium-activated chloride channel involved in fluid secretion, smooth muscle contraction, nociception and cancer progression.

Ani9 has been used to find out the inappropriate modulation of the membrane protein functions that are involved in the 198 ADGRG2- or Gq-mediated regulation of fluid reabsorption in the efferent ductules.

2-(4-chloro-2-methylphenoxy)-N-[(2-methoxyphenyl)methylideneamino]-acetamide (Ani9), the most potent inhibitor, is the structural analog of Ani7. It may be considered as a novel candidate for drug therapy of cancer, hypertension, pain, diarrhea and asthma.

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[1] YOHAN SEO. Ani9, A Novel Potent Small-Molecule ANO1 Inhibitor with Negligible Effect on ANO2.[J]. PLoS ONE, 2016: e0155771. DOI: 10.1371/journal.pone.0155771