生物活性

Thapsigargin is a cell-permeable sesquiterpene lactone found in the roots of Thapsia garganica. It is a tumor promoter and induces the release of intracellular stored Ca²⁺ without hydrolysis of inositolphospholipids via inhibition of the sarco/endoplasmic reticulum Ca²⁺-ATPase (SERCA; IC₅₀=30 nM). It may be used to distinguish between discrete intracellular Ca²⁺ pools. Thapsigargin-induced tumor promotion and down regulation of the EGF receptor is independent of protein kinase C activation.

体外研究

体内研究

激酶实验

细胞实验

动物实验

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Hakii H., et al. Thapsigargin, a histamine secretagogue, is a non-12-O-tetradecanolphorbol-13- acetate (TPA) type tumor promoter in two-stage mouse skin carcinogenesis. J Cancer Res Clin Oncol. 111 (3): 177–81 (1986).
[2] Davidson GA, et al. Kinetics of thapsigargin-Ca(2+)-ATPase (sarcoplasmic reticulum) inter- action reveals a two-step binding mechanism and picomolar inhibition. J Biol Chem. 270(20): 11731-4 (1995).
[3] Thastrup O, et al. Thapsigargin, a novel molecular probe for studying intracellular calcium release and storage. Agents Actions. 27(1-2):17-23 (1989).
[4] Inesi G, et al. Thapsigargin, a high affinity and global inhibitor of intracellular Ca2+ transport ATPases. Arch Biochem Biophys. 98(2):313-7 (1992).
[5] Treiman M, et al. A tool coming of age: thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca(2+)-ATPases. Trends Pharmacol Sci. 19(4):131-5 (1998).
[6] Jackisch C, et al. Delayed micromolar elevation in intracellular calcium precedes induction of apoptosis in thapsigargin-treated breast cancer cells. Clin Cancer Res. 6(7):2844-50 (2000).
[7] Ding WX, et al. Differential effects of endoplasmic reticulum stress-induced autophagy on cell survival. J Biol Chem. 282(7):4702-10 (2007).

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

相关化合物库

使用AMQUAR产品发表文献后请联系我们