Thapsigargin

SKU: orb2655651

Description

A potent, selective, non-competitive inhibitor of the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA), causes ER stress and induces autophagy in mammalian cells; inhibits the Ca2+ ATPase of rat liver ER about 100% at 170 nM, but no inhibition for skeletal muscle SR; increases the concentration of cytosolic free Ca2+ in sensitive cells by an acute and highly specific arrest of the endoplasmic reticulum Ca2+ pump.

Key Properties

• CAS Number: 67526-95-8
• MW: 650.76
• Purity: >98% (HPLC)
• Formula: C₃₄H₅₀O₁₂
• SMILES: CCCCCCCC(O[C@@H]1[C@@H](OC(/C(C)=C\C)=O)C(C)=C2[C@@]1([H])[C@@](C)(OC(C)=O)C[C@H](OC(CCC)=O)[C@@]([C@@]3(O)C)(O)[C@@]2([H])OC3=O)=O
• Target: Autophagy
• Solubility: In Vitro: DMSO : 50 mg/mL (76.83 mM)

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

G-202 | G 202 | G202

Quick Database Links

Gene Symbol

Autophagy