Thapsigargin
- 貨號 Cat. No.
- T-650
- 規格 Size
- 10 x 0.25 mg 0.65 mg 1mg 5mg 10mg
Description
Thapsigargin
An intracellular Ca2+ immobilizer
| Product#: | T-650 |
| Sizes: |
| 10 x 0.25 mg |
| 0.65 mg |
| 5 x 0.65 mg |
| 1 mg |
| 5 mg |
| 10 mg |
| M.W.: | 650.76 daltons. |
| CAS No.: | [67526-95-8] |
| Structure: |
| . |
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| Purity: | Greater than 99% by TLC. |
| Bioassay: |
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The biological activity was tested to confirm its ability to induce apoptosis in Jurkat cells. (above) Jurkat cells were grown to 70% confluency. Then 1 mM Thapsigargin or vehicle were added for 6 hours. At the end of the incubation period, the cells extracts were detected for cleaved Caspase 3 with Caspase 3 specific antibodies.
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Increasing intracellular Ca2+ by Thapsigargin modulates the autophosphorylation of Ca2+ Calmodolin Dependent Kinase II (CaMK II) in 3T3-L1 cells. (above) 3T3-L1 cells were starved for 2h and then stimulated with 1 or 5 mM Thapsigargin (#T-650) for the indicated times.The cell extracts were blotted and probed with an antibody for phospho-(Thr268)-CAMKII.
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Thapsigargin induced cytosolic Ca2+ increase in HEK 293 cells. (above) The graph above presents Ca2+ traces from Fluo-3 AM loaded HEK 293 cells treated with 5mM Thapsigargin in the presence of 5mM EGTA. |
| References: |
1. | Christensen, S. B. et al. (1980) Tetrahedron Lett. 21, 3829. |
2. | Christensen, S. B. et al. (1982) J. Org. Chem. 47, 649. |
3. | Rasmussen, U. et al. (1978) Acta Pharm. Suec. 15, 133. |
4. | Jackson, T. R. et al. (1988) Biochem. J. 253, 81. |
5. | Sagara, Y and Inesi, G. (1991) J. Biol. Chem. 266, 13503. |
6. | Lytton,J. et al. (1991) J. Biol. Chem., 266, 17067. |
7. | Takemura, H. et al. (1989) J. Biol. Chem. 264, 12266. |
8. | Rodriguez-Lopez, AM. et al. (1999) Cell Physiol Biochem. 9, 285. |
9. | Waring, P and Beaver, J. (1996) Exp Cell Res. 227, 264. |
10. | Wei, H. et al. (1998) J Neurochem, 70, 2305. |
11. | Patkar, S.A. (1979) Agents Actions 9, 53. |
12. | Ohuchi, K. et al. (1987) J. Cancer Res. Clin. Oncol. 113, 319. |
13. | Marks, F. et al. (1991) Carcinogensis 12, 1491. |
14. | Huber, M. et al. (2000) The Journal of Immunology 165, 124. |
15. | Chao, TS. et al. (1997) Cancer Research 57, 3168. |
Thapsigargin, derived from the plant genus Thapsia,1-3 is an extremely tight-binding inhibitor of intracellular Ca2+ pumps. It was initially described as a tumor promoting agent which induces rapid Ca2+ release from intracellular stores4 by inhibition of the sarcoplasmic/endoplasmic reticulm Ca2+-dependent ATPase pump without inositol phosphate formation.5-7 The thapsigargin induced depletion of Ca2+ stores causes apoptosis in most cell lines.8-10 It has also been shown to cause histamine secretion from rat mast cells,11 and to stimulate arachidonic acid metabolism in macrophages.12 Its tumour-promoting function probably results, at least partly, from cytotoxicity, causing a wound response in skin.13 The tumorogenic activity of thapsigargin might be due to its activation of protein kinase B (Akt) which subsequently stimulates MAP kinase signaling via Src and Raf-1.12,13