T16Ainh - A01 |
Catalog No.GC17930 |
아미노페닐티아졸인 T16Ainh - A01은 ~1μM의 IC50 값으로 TMEM16A 매개 염화물 전류를 억제하는 강력한 막횡단 단백질 16A(TMEM16A) 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 552309-42-9
Sample solution is provided at 25 µL, 10mM.
Transmembrane protein 16A (TMEM16A, also known as anoctamin-1) is a calcium-activated chloride channel (CaCC) with roles in transepithelial anion transport and smooth muscle contraction. T16A(inh)-A01 is an aminophenylthiazole that inhibits transient TMEM16A-mediated chloride currents with an IC50 value of ~1 µM.[1],[2] Its inhibitory effects are independent of voltage and do not prolong the rate of TMEM16A current deactivation.[2]T16A(inh)-A01 blocks CaCC activity in vascular smooth muscle cells and relaxes mouse and human blood vessels.[3] It also inhibits the proliferation of pancreatic cancer and squamous carcinoma cells in culture.[4],[5]
Reference:
[1]. Namkung, W., Phuan, P.W., and Verkman, A.S. TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloride channel conductance in airway and intestinal epithelial cells. The Journal of Biological Chemisty 286(3), 2365-2374 (2011).
[2]. Bradley, E., Fedigan, S., Webb, T., et al. Pharmacological characterization of TMEM16A currents. Channels 8(4), 308-320 (2014).
[3]. Davis, A.J., Shi, J., Pritchard, H.A.T., et al. Potent vasorelaxant activity of the TMEM16A inhibitor T16Ainh-A01. British Journal of Pharmacology 168, 773-784 (2013).
[4]. Mazzone, A., Eisenman, S.T., Strege, P.R., et al. Inhibition of cell proliferation by a selective inhibitor of the Ca2+ activated Cl- channel, Ano1. Biochemical and Biophysical Research Communications 427(2), 248-253 (2012).
[5]. Duvvuri, U., Shiwarski, D.J., Xiao, D., et al. TMEM16A induces MAPK and contributes directly to tumorigenesis and cancer progression. Cancer Research 72(13), 3270-3281 (2012).
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