T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC). Depolarization-evoked I ClCa in isolated RUICC, recorded using voltage clamp, were inhibited by T16Ainh-A01 with IC50 values of 3.4 μM. Eurogenic contractions of strips of rabbit urethra smooth muscle (RUSM), evoked by electric field stimulation (EFS), were also significantly reduced by T16Ainh-A01[1]. T16Ainh-A01 (10 μM) inhibits nearly completely TMEM16A chloride current (induced by 275 nM free calcium in the pipette) at all voltages, indicating a voltage-independent block mechanism[2]. T16Ainh-A01 led to the significant repression of cell proliferation, cell migration, and collagen secretion in CFs(cardiac fibroblasts)[3]. Suppression of ANO1 activity either by selective inhibitor (T16Ainh-A01) or by siRNA significantly attenuated the migration and invasion of ATC (Anaplastic thyroid carcinoma) cells[4].
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