ISOGINKGETIN

SKU: orb1222065

Description

Isoginkgetin, a compound derived from the leaves of Ginkgo biloba, to up-regulate adiponectin secretion with potency comparable to that of rosiglitazone, a known modulator of adiponectin production. Isoginkgetin has anti-tumor activity, the mechanistic basis is splicing inhibition , thus, pre-mRNA splicing inhibitors may represent a novel avenue for development of new anti-cancer agents.Isoginkgetin can inhibit tumor cell invasion by regulating phosphatidylinositol 3-kinase/Akt-dependent matrix metalloproteinase-9 expression. Isoginkgetin (0.3mg/kg ip for 3d) can reduce the level of O2·- in plasma and erythroeyte and sometimes increase the activity of SOD in anoxic rats, the action being stronger than aspirin.

Key Properties

• CAS Number: 548-19-6
• MW: 566.51
• Purity: >98% (HPLC)
• Formula: C₃₂H₂₂O₁₀
• SMILES: COC1=CC=C(C=C1)C2=CC(=O)C3=C(O2)C(=C(C=C3O)O)C4=C(C=CC(=C4)C5=CC(=O)C6=C(C=C(C=C6O5)O)O)OC
• Target: Others
• Solubility: DMSO : ≥ 83.3 mg/mL; 147.04 mM

Bioactivity

• In Vivo:
  Isoginkgetin (4 mg/kg; i.p.; daily for 14 days) shows anti-inflammatory effects. Animal model: Adult male Kunming mice (age 8–10weeks, 30–50 g). Dosage: 4 mg/kg. Administration: Daily for 14 days by intraperitoneally (i.p.) prior to LPS (0.83 mg/kg) administration. Result: Markedly suppressed the production of IL-1β, IL-6, tumor necrosis factor-alpha, cyclooxygenase-2, inducible nitric oxide, and reactive oxygen species.
• In Vitro:
  Isoginkgetin (0-20 μM, 24 h) inhibits cell invasion in a dose-dependent manner. Isoginkgetin (10 μM, 0-24 h) induces the accumulation of ubiquitinated protein cargo into perinuclear aggregates, activates autophagy and induces lysosomal swelling, repositioning, and acidification. Isoginkgetin (10 μM, 0-6 h) induces ER stress, impairs the unfolded protein response, and results in accumulation of ERAD substrates. Isoginkgetin directly inhibits the chymotrypsin-, trypsin-, and caspase-like activities of the 20S proteasome and impairs NF-κB signaling. Isoginkgetin (30 μM, 0-24 h) induces apoptosis in MM cell lines. Cell Invasion Assay Cell line: MDA-MB-231 and B16F10. Concentration: 0, 5, 10 and 20 μM. Incubation time: 24 h. Result: Inhibited cell invasion in a dose-dependent manner. Western blot analysis. Cell line: HeLa cells and MM cell lines (MM1S, 8826, OPM2, H929, JJN3 and U266). Concentration: 10 μM in HeLa cells, 30 μM in MM cell lines. Incubation time: 0-24 h. Result: Induced the expression of cleaved PARP-1 and Casp-3. Increased the protein levels of both ATF4 and ATF3. Decreased the level of LC3 I. Increased TFEB activation. Prevented the degradation of IκBα in response to stimulation with TNF-α. Cell Viability Assay Cell line: MM1S, 8826, OPM2, H929, JJN3 and U266 cells. Concentration: Incubation time: 72 h. Result: Inhibited cell viability with IC50 values of 3.992, 3.716, 4.749, 2.564, 3.806 and 4.147 μM against MM1S, 8826, OPM2, H929, JJN3 and U266 cells, respectively.

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

Isoginkgetin | IGG

Quick Database Links

Gene Symbol

Others