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Wedelolactone

SKU: orb1224805

Description

Wedelolactone inhibits adipogenic differentiation through ERK pathway, may be a novel inhibitory effect on adipogenic differentiation in hAMSCs.(In Vitro):Wedelolactone (0-5 μg/mL; 0-21 d) enhances bone marrow mesenchymal stem cells (BMSC) differentiation towards osteoblasts.Wedelolactone (0-6 μg/mL; 0-9 d) inhibits GSK3β activity and increases β-catenin and runx2 nuclear accumulation in BMSC, and inhibits the effect of RANKL.Wedelolactone (0-5 μg/ml; 60 min) inhibits GSK3β activity and proves GSK3β is the target of wedelolactone.Wedelolactone (0-5 μg/ml; 6 d) inhibits c-src, c-fos and cathepsin k expression level.(In Vivo):Wedelolactone (10 mg/kg; i.p. every 2 days for 4 weeks) decreases bone volumn and trabecular number at the femur after ovarietomy, and prevents the VOX-induced bone loss.

Images & Validation

Key Properties

CAS Number524-12-9
MW314.3
Purity>98% (HPLC)
FormulaC16H10O7
SMILESO=C1C2=C(OC3=CC(O)=C(O)C=C32)C4=C(O)C=C(OC)C=C4O1
TargetNF-κB
SolubilitySoluble in Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.

Bioactivity

In Vivo
Wedelolactone (10 mg/kg; i.p. every 2 days for 4 weeks) decreases bone volumn and trabecular number at the femur after ovarietomy, and prevents the VOX-induced bone loss. Animal model: Ovariectomized 9-week-old mice. Dosage: 10 mg/kg. Administration: Intraperitoneal injection; 10 mg/kg every 2 days; for 4 weeks. Result: Inhibited osteoclast activity and stimulated osteoblast differentiation to achieved osteoprotective effect.
In Vitro
Wedelolactone (0-5 μg/mL; 0-21 d) enhances bone marrow mesenchymal stem cells (BMSC) differentiation towards osteoblasts. Wedelolactone (0-6 μg/mL; 0-9 d) inhibits GSK3β activity and increases β-catenin and runx2 nuclear accumulation in BMSC, and inhibits the effect of RANKL. Wedelolactone (0-5 μg/ml; 60 min) inhibits GSK3β activity and proves GSK3β is the target of wedelolactone. Wedelolactone (0-5 μg/ml; 6 d) inhibits c-src, c-fos and cathepsin k expression level. Cell Differentiation Assay Cell line: Mouse BMSC. Concentration: 0-5 μg/mL. Incubation time: 0, 6, 9, 12 and 21 days. Result: Increased Mouse BMSC into osteoblastic cells and dose-dependently increased the activity of alkaline phosphatase at incubation for 9 days. Western blot analysis. Cell line: Mouse BMSC and RAW264.7 cells Concentration: 0-5 μg/mL. Incubation time: 0-9 days. Result: Decreased GSK3β expression level and up-regulated GSK3β phosphorylation, nuclear accumulation of β-catenin and runx2 in BMSC. Inhibited RANKL-induced phosphorylation of NF-κB/p65 and the expression level of c-fos and c-Src. Cell Viability Assay Cell line: Mouse BMSC. Concentration: 0.1, 1.25, 2.5, 5 μg/ml Incubation time: 60 min. Result: Inhibited GSK3β activity with an IC50 of 21.7 μM weeker than staurosporin which is a GSK3β inhibitor and proved GSK3β is a target. RT-PCR Cell line: RAW264.7 cells Concentration: 0, 0.6, 1.25, 2.5 and 5 μg/mL Incubation time: 6 days. Result: Inhibited the expression of osteoclast differentiation related marker genes c-src, c-fos and cathepsin in RAW264.7 cells.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

IKK Inhibitor II

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5 mg
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