BAY 11-7085

SKU: orb1225779

Description

An inhibitor of the expression of ICAM-1, VCAM-1, and E-selectin in human endothelial cells (IC50=5-10 uM); acts by selectively inhibiting TNFα-induced phosphorylation of IκB-α without affecting the constitutive IκB-α phosphorylation; prevents PMA-induced NF-kappaB nuclear translocation; reduces swelling in both the rat carrageenan paw edema assay and in a rat adjuvant arthritis model.

Key Properties

• CAS Number: 196309-76-9
• MW: 249.3287
• Purity: >98% (HPLC)
• Formula: C₁₃H₁₅NO₂S
• SMILES: N#C/C=C/S(=O)(C1=CC=C(C(C)(C)C)C=C1)=O
• Target: NF-κB
• Solubility: DMSO: ≥ 26 mg/mL

Bioactivity

• In Vivo:
  BAY 11-7085 acts as an anti-inflammatory agent in both the rat carrageenan paw and the rat adjuvant arthritis model. It demonstrates a dose-dependent reduction in swelling in the rat carrageenan paw model.
• In Vitro:
  BAY 11-7085 inhibits TNFa-induced surface expression of E-selectin, VCAM-1, and ICAM-1with IC50 values in the range of 5-10 μM. BAY 11-7085 stabilizes IκBα in a dose-dependent manner with an IC50 value of approximately 10 μM. There is a clear correlation between the concentration of drug that stabilized IκBα, the concentration that inhibits nuclear levels of NF-kB, and the concentration that inhibits adhesion molecule expression. BAY 11-7085 has been shown to inhibit cell proliferation and induce apoptosis of a variety of cells. BAY 11-7085 (ECSCs) significantly inhibits the cell proliferation and DNA synthesis of ovarian endometriotic cyst stromal cells and induces apoptosis and the G0/G1 phase cell cycle arrest of these cells. BAY 11-7085 induces apoptosis of ECSCs by suppressing antiapoptotic proteins, and that caspase-3-, -8-, and -9-mediated cascades are involved in this mechanism.

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

BAY11-7085 | BAY-11-7085 | BAY 11-7083

Quick Database Links

Gene Symbol

NF-κB