Ani 9 is a highly selective inhibitor of ANO1 that potently blocks ANO1 channel activity with an IC₅₀ below 3μM. Ani 9 did not affect the intracellular calcium signaling and CFTR chloride channel activity. Ani 9 may be a useful pharmacological tool for studying ANO1 and a potential development candidate for drug therapy of cancer, hypertension, pain, diarrhea and asthma[1].
In vitro, treatment with 3-30μM Ani 9 for 24-72h inhibited PC-3 cell growth in dose-dependent and time-dependent manner[2]. Application of Ani 9 up to 30μM for 20min did not affect the ATP-induced cytosolic calcium increase in FRT cells[1]. 1μM, 3μM and 10μM Ani 9 for 20min inhibited VRAC activity by 13.5±1.1%, 21.4±1.0% and 40.7±1.5%, respectively in LN215[1]. 3μM Ani9 for 30min did not affect electrical field stimulation (EFS)-evoked contractions of male murine USM[3]. 10μM Ani 9 for 30min had no blocking effect on contractures of mouse bronchi induced by carbachol[4].
References:
[1] Seo Y, Lee HK, Park J, et al. Ani9, A Novel Potent Small-Molecule ANO1 Inhibitor with Negligible Effect on ANO2. PLoS One. 2016;11(5):e0155771.
[2] Song Y, Gao J, Guan L, Chen X, Gao J, Wang K. Inhibition of ANO1/TMEM16A induces apoptosis in human prostate carcinoma cells by activating TNF-α signaling. Cell Death Dis. 2018;9(6):703.
[3] Gupta N, Baker SA, Sanders KM, et al. ANO1 channels are expressed in mouse urethral smooth muscle but do not contribute to agonist or neurally evoked contractions. Sci Rep. 2025;15(1):17365.
[4] Dwivedi R, Drumm BT, Alkawadri T, et al. The TMEM16A blockers benzbromarone and MONNA cause intracellular Ca2+-release in mouse bronchial smooth muscle cells. Eur J Pharmacol.
Ani 9是一种高选择性的ANO1抑制剂，可有效阻断ANO1通道活性，对ANO1的IC₅₀值小于3μM。Ani 9不影响细胞内钙信号传导和CFTR氯离子通道活性。Ani 9可能是一种有用的药理学工具，用于研究ANO1，并有望成为治疗癌症、高血压、疼痛、腹泻和哮喘的潜在药物候选物[1]。
体外实验中，3-30μM的Ani 9处理PC-3细胞24-72小时，PC-3细胞的活性以剂量依赖和时间依赖的方式被抑制[2]。30μM的Ani 9处理FRT细胞20分钟，不影响ATP诱导的细胞质钙升高[1]。在LN215细胞中，1μM、3μM和10μM的Ani 9处理20分钟，对VRAC的活性抑制率分别在13.5±1.1%、21.4±1.0%和40.7±1.5%[1]。3μM的Ani 9处理30分钟，不影响电场刺激（EFS）诱导的雄性小鼠尿道平滑肌的收缩[3]。10μM的Ani 9处理30分钟，对卡巴胆碱诱导的小鼠支气管收缩没有阻断作用[4]。