Bay 11-7085

Bay 11-7085, a soluble inhibitor of NK-kappaB activation, has been shown to inhibit cell proliferation and induce apoptosis of a variety of 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. Bay 11-7085 could be used as a therapeutic agent for the treatment of endometriosis. Bay 11-7085 protects against gut ischemia-reperfusion injury.

Product information

CAS Number: 196309-76-9

Molecular Weight: 249.33

Formula: C13H15NO2S

Synonym:

Bay 11-7085

Bay-11-7085

Bay11-7085

Bay-117085

Chemical Name: (2E)-3-[[4-(1,1-Dimethylethyl)phenyl]sulfonyl]-2-propenenitrile

Smiles: CC(C)(C)C1C=CC(=CC=1)S(=O)(=O)/C=C/C#N

InChiKey: VHKZGNPOHPFPER-ONNFQVAWSA-N

InChi: InChI=1S/C13H15NO2S/c1-13(2,3)11-5-7-12(8-6-11)17(15,16)10-4-9-14/h4-8,10H,1-3H3/b10-4+

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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.

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.

References:

1. Relic B, Charlier E, Deroyer C, Malaise O, Neuville S, Desoroux A, Gillet P, de Seny D, Malaise MG. Bay11-7085 induces glucocorticoid receptor activation and autophagy that collaborate with apoptosis to induce human synovial fibroblast cell death. Oncotarget. 2016 Apr 26;7(17):23370-82. doi: 10.18632/oncotarget.8042. PubMed PMID: 26993765; PubMed Central PMCID: PMC5029633.
2. Berger N, Ben Bassat H, Klein BY, Laskov R. Cytotoxicity of NF-kappaB inhibitors Bay 11-7085 and caffeic acid phenethyl ester to Ramos and other human B-lymphoma cell lines. Exp Hematol. 2007 Oct;35(10):1495-509. PubMed PMID: 17889719.
3. Nasu K, Nishida M, Ueda T, Yuge A, Takai N, Narahara H. Application of the nuclear factor-kappaB inhibitor Bay11-7085 for the treatment of endometriosis: an in vitro study. Am J Physiol Endocrinol Metab. 2007 Jul;293(1):E16-23. PubMed PMID: 16896168.
4. Relic B, Benoit V, Franchimont N, Kaiser MJ, Hauzeur JP, Gillet P, Merville MP, Bours V, Malaise MG. Peroxisome proliferator-activated receptor-gamma1 is dephosphorylated and degraded during Bay11-7085-induced synovial fibroblast apoptosis. J Biol Chem. 2006 Aug 11;281(32):22597-604. PubMed PMID: 16766531.
5. Hernandez-Gutierrez S, Garcia-Pelaez I, Zentella-Dehesa A, Ramos-Kuri M, Hernandez-Franco P, Hernandez-Sanchez F, Rojas E. NF-kappaB signaling blockade by Bay 11-7085 during early cardiac morphogenesis induces alterations of the outflow tract in chicken heart. Apoptosis. 2006 Jul;11(7):1101-9. PubMed PMID: 16699956.

Products are for research use only. Not for human use.