Gigantol

SKU: orb1221890

Description

Gigantol is a novel inhibitor of the Wnt/β-catenin pathway. It inhibits Wnt/β-catenin signaling through downregulation of phosphorylated LRP6 and cytosolic β-catenin in breast cancer cells. Gigantol may be developed as a promising neuroprotective agent for successful MSC transplantation in ischemic diseases, it shows the protective effect against hydrogen peroxide-induced apoptosis in rat bone marrow mesenchymal stem cells through the PI3K/Akt pathway.Gigantol inhibits aldose reductase gene to exert its anti-cataract activity. Gigantol induces growth inhibition and apoptosis of HepG2 cells via the PI3K/Akt/NF-κB signaling pathway.Gigantol also shows α-glucosidase inhibitory activity.

Key Properties

• CAS Number: 67884-30-4
• MW: 274.31
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₈O₄
• SMILES: COc1cc(O)cc(CCc2ccc(OC)c(O)c2)c1
• Target: β-catenin| α-glucosidase
• Solubility: DMSO : ≥ 160 mg/mL; 583.28 mM

Bioactivity

• In Vivo:
  LDD and Gigantol isomer-1 (25–100 mg/kg, p.o.) significantly increase the hot-plate latency in comparison to vehicle-treated mice and decreased carrageenaninduced inflammation in rats.
• In Vitro:
  Gigantol isomer-1 decreases the level of phosphorylated LRP6 and cytosolic β-catenin in HEK293 cells. In breast cancer MDA-MB-231 and MDA-MB-468 cells, treatment with Gigantol isomer-1 reduces the level of phosphorylated LRP6. Gigantol isomer-1 significantly inhibits the proliferation and induces apoptosis of the HepG2 cells. Gigantol isomer-1 at concentrations of 1, 40 and 150 μM markedly decreases the cell viability by 11.7, 30.0 and 56.4% at 24 h and 21.1, 66.8 and 85.5% at 48 h, respectively. The IC50 value is 9.30 μM.

Storage & Handling

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

Quick Database Links

Gene Symbol

β-catenin| α-glucosidase