67526-95-8
物理化學(xué)性質(zhì)
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Target | Value |
SERCA
() |
Thapsigargin (0.001-?1 μM; for 2 and 4 days) arrests cell proliferations in MH7A human rheumatoid arthritis synovial cells in a time- and dose-dependent manner.
Thapsigargin (0.001-?1 μM; for 2 and 4 days) induces cell apoptosis in MH7A cells in a time- and dose-dependent manner.
Thapsigargin (0.001-?1 μM; for 2 and 4 days) impairs mTOR activity and leads to cyclin D1 expressions in MH7A cells.
Thapsigargin inhibits Ca
2+
entry into human neutrophil granulocytes.
Thapsigargin inhibits the carbachol-evoked [Ca
2+
]i-transients with (IC
50
=0.353 nM) or without (IC
50
=0.448 nM) a KCl-prestimulation, but an additional small component, with a much lower sensitivity (IC
50
=4814 nM), is observed in the absence of a KCl-prestimulation. In contrast, the KCl-evoked [Ca
2+
]i-transients displayed only one component with a very low sensitivity to Thapsigargin in both absence (IC
50
=3343 nM) and presence (IC
50
=6858 nM) of a carbachol-prestimulation.
Cell Proliferation Assay
Cell Line: | MH7A human rheumatoid arthritis synovial cells |
Concentration: | 0.001, 0.1, and 1?μM |
Incubation Time: | For 2 and 4 days |
Result: | Arrested cell proliferations in a time- and dose-dependent manner. |
Apoptosis Analysis
Cell Line: | MH7A human rheumatoid arthritis synovial cells |
Concentration: | 0.001, 0.1, and 1?μM |
Incubation Time: | For 2 and 4 days |
Result: | Induces cell apoptosis in a time- and dose-dependent manner. |
Western Blot Analysis
Cell Line: | MH7A human rheumatoid arthritis synovial cells |
Concentration: | 0.001, 0.1, and 1?μM |
Incubation Time: | For 2 and 4 days |
Result: | Impairs mTOR activity and leads to cyclin D1 expressions |
Thapsigargin (Injection; 0.25 ug/g, 0.5 ug/g and 1 ug/g; 24 hours) significant increases of 2 to 5-fold in chemokine and pro-inflammatory expression. Thapsigargin is more sensitive to inducing a systemic immune response.
Animal Model: | Male Balb/c mice (20-25 g) |
Dosage: | 0.25 ug/g, 0.5 ug/g and 1 ug/g |
Administration: | Injection; 24 hours |
Result: | Increased of 2 to 5-fold in chemokine and pro-inflammatory expression. |