耗材描述
Thapsigargin
产品活性:Thapsigargin,内质网应激诱导剂, 是一种微粒体 Ca2+-ATPase 抑制剂。Thapsigargin 能有效抑制不同细胞类型的病毒 (HCoV-229E、MERS-CoV、COVID-19) 复制。
产品来源: https://www.medchemexpress.cn/Thapsigargin.html
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling | Anti-infection | Apoptosis
作用靶点:Calcium Channel | SARS-CoV | Apoptosis
来源:植物 | 伞形科 | 毒胡萝卜
结构分类:萜类 | 二萜
In Vitro: 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 Ca2+ entry into human neutrophil granulocytes.
Thapsigargin inhibits the carbachol-evoked [Ca2+]i-transients with (IC50=0.353 nM) or without (IC50=0.448 nM) a KCl-prestimulation, but an additional small component, with a much lower sensitivity (IC50=4814 nM), is observed in the absence of a KCl-prestimulation. In contrast, the KCl-evoked [Ca2+]i-transients displayed only one component with a very low sensitivity to Thapsigargin in both absence (IC50=3343 nM) and presence (IC50=6858 nM) of a carbachol-prestimulation.
Thapsigargin also phosphorylate p38 MAPK by Ca2+ influx through SOCE, leading to suppression of TNF-α-induced NF-κB phosphorylation.
In Vivo: 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.
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