Ginkgetin

SKU: orb1222202

Description

Ginkgetin has anti-influenza virus and anti-fungal activities. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. Ginkgetin is a good STAT3 inhibitor and may be a useful lead molecule for development of a therapeutic STAT3 inhibitor. Ginkgetin induces apoptosis in PC-3 cells via activation of caspase 3 and inhibition of survival genes as a potent chemotherapeutic agent for prostate cancer treatment. Ginkgetin has neuroprotective activity against neurological injury induced by MPTP occurs via regulating iron homeostasis, it may provide neuroprotective therapy for Parkinson's disease and iron metabolism disorder related diseases.

Key Properties

• CAS Number: 481-46-9
• MW: 566.51
• Purity: >98% (HPLC)
• Formula: C₃₂H₂₂O₁₀
• SMILES: COC1=C(C=C(C=C1)C2=CC(=O)C3=C(C=C(C=C3O2)OC)O)C4=C(C=C(C5=C4OC(=CC5=O)C6=CC=C(C=C6)O)O)O
• Target: CaMK
• Solubility: DMSO : ≥ 83.3 mg/mL; 147.04 mM

Bioactivity

• In Vivo:
  Ginkgetin (25-100 mg/kg; i.p. 2 hours after the onset of ischemia) exerts anti-inflammatory effects on cerebral ischemia/reperfusion-induced injury in a rat model via the TLR4/NF-κB signaling pathway. Ginkgetin (30 mg/kg; intragastrically once per day for 42 d) suppresses tumor growth in A549 cells bearing nude mice. Animal model: Male Sprague-Dawley rats (200-220 g). Dosage: 25, 50, 100 mg/kg. Administration: i.p. 2 hours after the onset of ischemia. Result: Reduced the neurological de cit score. Suppressed the expression of NF-κB, TLR4 and IκBαin ischemic penumbra cortex, and inhibited the degradation of IκBα. Decreased the expressions of ICAM-1, COX-2, and iNOS. Downregulated downstream in ammatory factor PGE2 and TNF-α expression. Decreased IL-1β, IL-6, IL-8, and IL-10 protein expression.
• In Vitro:
  Ginkgetin (2.5-20 μM; 48 h) inhibits the growth of Daoy and D283 cell lines, and induces G2/M cell cycle arrest in Daoy cells. Ginkgetin (20-40 μM; 24 h) significantly activates the apoptosis of osteosarcoma cells in a concentration-dependent manner. Ginkgetin (10-20 μM; 3-24 h) down-regulated the expression of Wnt target genes without affecting the expression of β-catenin in medulloblastoma cells. Ginkgetin (1-10 μM; 24 or 48 h) significantly inhibits the VEGF-induced endothelial cell proliferation, migration, and wound recovery in a concentration-dependent manner. Ginkgetin (5-10 μM; 48 h) induces autophagy responsible for cell death in A549.Cell Viability Assay Cell line: Daoy and D283 cell lines. Concentration: 2.5, 5, 10, 20 μM Incubation time: 48 hours. Result: Inhibited the cell growth, with IC50s of 14.65 and 15.81 μM for Daoy and D283 cells, respectively. Apoptosis Analysis Cell line: Osteosarcoma cells. Concentration: 20, 30, 40 μM. Incubation time: 24 hours. Result: Markedly induced the apoptosis of osteosarcoma cells in a concentration-dependent manner. Cell Cycle Analysis Cell line: Daoy cells. Concentration: 2.5, 5, 10, 20 μM Incubation time: 24 hours. Result: Increased G2/M phase, compared with that of control, indicating a G2/M cell phase arrest. Cell Cycle Analysis Cell line: Daoy and D283 cell lines. Concentration: 10, 20 μM. Incubation time: 3, 6, 12, 24 hours. Result: Attenuated the expression of Wnt target genes, Axin2, cyclin D1 and survivin at 20 μM for 24 h in Daoy cells. Unaffected the level of total β-catenin and diminished the level of β-catenin phosphorylation in a time- and concentration-dependent manner.

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

Ginkgetin

Quick Database Links

Gene Symbol

CaMK