Mollugin

SKU: orb1222045

Description

Mollugin may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.

Key Properties

• CAS Number: 55481-88-4
• MW: 284.3
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₆O₄
• SMILES: CC1(C=Cc2c(O1)c1ccccc1c(c2C(=O)OC)O)C
• Target: COX
• Solubility: In Vitro: DMSO : 33.33 mg/mL (117.23 mM)

Bioactivity

• In Vivo:
  Mollugin (0-75 mg/kg, Orally, three times per week for 36 days) inhibits growth of HeLa cells in a xenograft tumor model. Animal model: BALB/c female athymic nude mice (six-week-old, subcutaneously injected with 0.2 mL HeLa cells). Dosage: 0, 25 and 75 mg/kg. Administration: Orally, three times per week for 36 days. Result: Suppressed tumor growth, whereas the body weight did not change. Significantly reduced the protein expression of p-p65 and COX-2 in the tumors.
• In Vitro:
  Mollugin (0-80 μM, 24 h) inhibits the expression of an NF-κB reporter gene induced by TNF-α in a dose-dependent manner. Mollugin (0-80 μM, 12 h) inhibits the proliferation of HeLa cells. Mollugin (0-80 μM, 12 h) inhibits TNF-α-induced phosphorylation and nuclear translocation of p65, phosphorylation and degradation of IκBα, and IKK phosphorylation, and inhibits the TNF-α-induced mRNA expression of Cyclin D1, c-Myc, and VEGF. Mollugin (0-80 μM, 12 h) enhances TNF-α-induced apoptosis. Cell Viability Assay Cell line: HeLa, Hep3B, and HEK293 cells. Concentration: 0, 10, 20, 40, and 80 μM. Incubation time: 24 h. Result: Significantly inhibited NF-κB reporter gene expression in a dose-dependent manner, did not display significant cellular toxicity in HeLa, Hep3B, and HEK293 cells. Cell Proliferation Assay Cell line: HeLa cells. Concentration: 0, 20, 40, and 80 μM. Incubation time: 12 h. Result: Inhibited the proliferation of HeLa cells. Apoptosis Analysis Cell line: HeLa cells. Concentration: 0, 10, 20, 40, and 80 μM. Incubation time: 12 h. Result: Slightly affected the caspase-3 activation, potentiated the effect of TNF-α-induced PARP cleavage, and enhanced the apoptotic effects of TNF-α. Western blot analysis. Cell line: HeLa cells. Concentration: 0, 10, 20, 40, and 80 μM. Incubation time: 12 h. Result: Significantly inhibited the TNF-α-induced p65 phosphorylation and block TNF-α-induced nuclear translocation of p65 in a dose-dependent manner, completely inhibited degradation of IκBα at 80 μM, and abolished the TNF-α-induced IKK phosphorylation at 80 μM. Inhibited the TNF-α-induced mRNA expression of Cyclin D1, c-Myc, and VEGF at 80 μM.

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

Rubimaillin | Mollugin

Quick Database Links

Gene Symbol

COX