Thapsigargin

SKU: orb1296066

Description

Thapsigargin is a natural SERCA inhibitor that disrupts calcium homeostasis by blocking Ca2+ uptake into the ER/SR, leading to elevated cytosolic Ca2+ and ER stress. It is widely used in vitro and in vivo to study apoptosis, autophagy, and ER stress signaling pathways in cancer and neurodegenerative disease research.

Research Area

Cell Biology

Key Properties

• CAS Number: 67526-95-8
• MW: 650.77
• Purity: >98%
• Formula: C₃₄H₅₀O₁₂
• SMILES: O(C(CCCCCCC)=O)[C@H]1[C@]2(C([C@]3([C@](O)([C@@H](OC(CCC)=O)C[C@@]2(OC(C)=O)C)[C@](C)(O)C(=O)O3)[H])=C(C)[C@@H]1OC(/C(=C\C)/C)=O)[H]
• Target: ATPase
• Solubility: Soluble in DMSO (up to 65 mg/ml) or in Ethanol (up to 20 mg/ml).

Bioactivity

• Target IC50:
  PC3 cells:2.4 μM|CCRF S-180 cells:30 nM|K562 cells:0.17 μM|CCRF-CEM cells:0.27 μM|MCF-7 cells:2.3 μM|EL4 cells:0.1 μM|HL-60 cells:0.007 μM
• In Vivo:
  METHODS: To assay in vivo ER stress-inducing activity, Thapsigargin (0.25-1 μg/g in 150 mM dextrose containing 1% DMSO) was administered as a single intraperitoneal injection to Balb/c mice in order. RESULTS: Thapsigargin treatment resulted in significant expression of the ER stress markers ATF6 and eIF2α in adipose tissue. thapsigargin treatment failed to induce the expression of most of the ER stress and UPR proteins in the liver. METHODS: To investigate the antiviral function in vivo, Thapsigargin (30 ng/mouse) was administered by gavage to PR8 virus-infected BALB/c mice once daily for seven days. RESULTS: Oral administration of Thapsigargin to mice significantly reduced severity and viral shedding and improved survival during infection with the deadly influenza virus.
• In Vitro:
  METHODS: Human rheumatoid arthritis synoviocytes MH7A were treated with Thapsigargin (0.001-1 μM) for 2-4 days, and cell proliferation was detected using the SRB. RESULTS: Thapsigargin inhibited the proliferation of MH7A cells in a time- and dose-dependent manner. METHODS: Human hepatocellular carcinoma cells HepG2 were treated with Thapsigargin (25-100 nM) for 24 h. Endoplasmic reticulum stress/UPR gene expression was detected by RT-qPCR. RESULTS: Thapsigargin treatment consistently induced ER stress gene expression only at elevated concentrations of 50 and 100 nM.
• Cell Research:
  Cell Line: MH7A human rheumatoid arthritis synovial cells. Concentration: 0.001, 0.1, and 1 μM. Incubation Time: For 2 and 4 days
• Animal Research:
  Animal Model: Male Balb/c mice (20-25g). Dosage: 0.25ug/g, 0.5ug/g and 1ug/g. Administration: Injection; 24 hours

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

unfolded, protein ,response, SARSCoV, SARS coronavirus, SARS-CoV, stress, Thapsigargin, inhibit, Inhibitor, Apoptosis, CalciumChannel, Ca2+ channels, Ca2+-ATPase, Calcium Channel, Ca channels, coronavirus

Compound Identifiers

PubChem CID

49926