thapsigargin

Thapsigargin is a **naturally occurring sesquiterpene lactone** isolated from the plant *Thapsia garganica*. It acts as a **non-competitive, irreversible inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump**, leading to depletion of endoplasmic reticulum calcium stores, increased cytosolic calcium concentration, endoplasmic reticulum (ER) stress, and ultimately **apoptosis (programmed cell death)**[1][3][4][5][7][9]. Thapsigargin inhibition of SERCA triggers the unfolded protein response and can block autophagy[1][4]. Due to its high cytotoxicity and non-specific cell killing, it is primarily used in laboratory research and as a tool compound, not as a marketed pharmaceutical drug. Thapsigargin and its prodrugs (such as mipsagargin) have been investigated for **anticancer activities** in various preclinical models and early-phase clinical trials, but the use of thapsigargin as a therapeutic agent is limited by severe toxicity[3][7][9]. The compound has also been noted to induce a potent antiviral host response in experimental settings[2][4]. In research, it is widely used to study calcium signaling, ER stress, apoptosis, and autophagy.

Other names

TGthapsigarginCa2+-ATPase inhibitorhapsigarginThapsigargin (TG)