Thapsigargin is a specific inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+-ATPase (SERCA). Thapsigargin increases cytosolic calcium levels through release from intracellular calcium stores. Depletion of ER calcium stores leads to Ca2+ influx via activation of store (voltage)-operated calcium channels in the plasma membrane, mediating numerous physiological functions, including exocytosis, chemotaxis, transcription, cell division, and apoptosis. There are preclinical indications that the drug may have anticancer potential.
According to a recent paper Thapsigargin indirectly and robustly inhibits nonsense-mediated RNA decay (NMD), and this potential of thapsigargin has been harnessed to develop a method that detects NMD efficiency inside the cell.
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