Description
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:
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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.
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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.
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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.
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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.
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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.
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