CaCCInh-A01 | TMEM16A inhibitor

CaCCInh-A01 chemical structure

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CaCCInh-A01 (407587-33-1) is a potent inhibitor of TMEM16A (IC50 = 2.1 mM), a calcium-activated chloride channel1. Blockade of TMEM16A with CaCCInh-A01 protects against renal fibrosis2, reduces blood brain barrier permeability, attenuates brain infarct size and neurological deficits after ischemic stroke3, and induces apoptosis and cell cycle arrest in various epithelium-originated cancer cells4.

References/Citations:

  1. 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
  2. Li et al. (2022) Blockade of TMEM16A protects against renal fibrosis by reducing intracellular Cl– concentration; Br. J. Pharmacol. 179 3043
  3. Liu et al. (2019) TMEM16A Inhibition Preserves Blood-Brain Barrier Integrity After Ischemic Stroke; Front. Cell Neurosci. 13 360
  4. Guan et al. (2016) Inhibition of calcium-activated chloride channel ANO1 suppresses proliferation and induces apoptosis of epithelium originated cancer cells; Oncotarget 7 78619
407587-33-1, CaCCInh-A01, CaCCInh-A01 supplier, CaCCInhA01, TMEM16A inhibitor

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CaCCInh-A01 (407587-33-1) is a potent inhibitor of TMEM16A (IC50 = 2.1 mM), a calcium-activated chloride channel1. Blockade of TMEM16A with CaCCInh-A01 protects against renal fibrosis2, reduces blood brain barrier permeability, attenuates brain infarct size and neurological deficits after ischemic stroke3, and induces apoptosis and cell cycle arrest in various epithelium-originated cancer cells4.

References/Citations:

  1. 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
  2. Li et al. (2022) Blockade of TMEM16A protects against renal fibrosis by reducing intracellular Cl– concentration; Br. J. Pharmacol. 179 3043
  3. Liu et al. (2019) TMEM16A Inhibition Preserves Blood-Brain Barrier Integrity After Ischemic Stroke; Front. Cell Neurosci. 13 360
  4. Guan et al. (2016) Inhibition of calcium-activated chloride channel ANO1 suppresses proliferation and induces apoptosis of epithelium originated cancer cells; Oncotarget 7 78619