Bay 11-7085

Cas：196309-76-9

Product Information：

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.

Chemical Formula: C13H15NO2S

Exact Mass: 249.08235

Molecular Weight: 249.33

Elemental Analysis: C, 62.63; H, 6.06; N, 5.62; O, 12.83; S, 12.86

Synonym: 

Bay 11-7085

Bay-11-7085

Bay11-7085

Bay 117085

Bay-117085

Bay117085

Chemical Name:

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

InChi Key:

VHKZGNPOHPFPER-ONNFQVAWSA-N

InChi Code:

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+

Smiles Code:

N#C/C=C/S(=O)(C1=CC=C(C(C)(C)C)C=C1)=O

Technical Data：

Appearance: White to off white solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

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.