| Description | Thapsigargin is a natural product, an inhibitor of sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum. |
| In vitro | 方法：人类风湿性关节炎滑膜细胞 MH7A 用 Thapsigargin (0.001-1 μM) 处理 2-4 天，使用 SRB 方法检测细胞增殖。结果：Thapsigargin 以时间和剂量依赖的方式抑制 MH7A 细胞的增殖。[1]方法：人肝癌细胞 HepG2 用 Thapsigargin (25-100 nM) 处理 24 h，使用 RT-qPCR 检测内质网应激/UPR 基因表达。结果：Thapsigargin 治疗仅在 50 和 100 nM 的升高浓度下持续诱导ER应激基因表达。[2] |
| In vivo | 方法：为检测体内诱导 ER 应激的活性，将 Thapsigargin (0.25-1 μg/g in 150 mM dextrose containing 1% DMSO) 单次腹腔注射给 Balb/c 小鼠。结果：Thapsigargin 治疗导致脂肪组织中 ER 应激标记物 ATF6 和 eIF2α 的显著表达。Thapsigargin 治疗未能诱导肝脏中大多数 ER 应激和 UPR 蛋白的表达。[2]方法：为研究在体内的抗病毒功能，将 Thapsigargin (30 ng/mouse) 灌胃给药给感染 PR8 病毒的 BALB/c 小鼠，每天一次，持续七天。结果：小鼠口服 Thapsigargin 显著降低了严重程度和病毒脱落，并提高了致命流感病毒感染期间的存活率。[3] |
| Cell experiments | Cell Line: MH7A human rheumatoid arthritis synovial cells. Concentration: 0.001, 0.1, and 1?μM. Incubation Time: For 2 and 4 days [2] |
| Animal experiments | Animal Model: Male Balb/c mice (20-25g). Dosage: 0.25ug/g, 0.5ug/g and 1ug/g. Administration: Injection; 24 hours [4] |
| Synonyms | 毒胡萝卜素 |
| molecular weight | 650.75 |
| Molecular formula | C34H50O12 |
| CAS | 67526-95-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (69.15 mM), Sonication is recommended. |
| References | 1. Wang H, et al. Effects of thapsigargin on the proliferation and survival of human rheumatoid arthritis synovial cells. ScientificWorldJournal. 2014 Feb 9;2014:605416. 2. Abdullahi A, et al. Modeling Acute ER Stress in Vivo and in Vitro. Shock. 2017 Apr;47(4):506-513. 3. Goulding LV, et al. Thapsigargin at Non-Cytotoxic Levels Induces a Potent Host Antiviral Response that Blocks Influenza A Virus Replication. Viruses. 2020 Sep 27;12(10):1093. 4. Abdullahi A, et al. Modeling Acute ER Stress in Vivo and in Vitro. Shock. 2017 Apr;47(4):506-513. |