Bay 11-7085

An irreversible inhibitor of IκBα phosphorylation

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10mg

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货号: ajci4932
CAS: 196309-76-9
别名: (2E)-3-[[4-叔丁基苯基]磺酰基]-2-丙烯腈,BAY 11-7083
分子式: C13H15NO2S
分子量: 249.33
纯度: >98%
溶解度: ≥ 12.45mg/mL in DMSO
储存: Store at -20° C
库存: 现货

Background

BAY 11-7085 is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM.

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[1]. 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[2].

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[1].

参考文献:
[1]. Pierce JW, et al. Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesionmolecule expression show anti-inflammatory effects in vivo. J Biol Chem. 1997 Aug 22;272(34):21096-103.
[2]. Nasu K, et al. Application of the nuclear factor-kappaB inhibitor BAY 11-7085 for the treatment of endometriosis: an in vitro study. Am J Physiol Endocrinol Metab. 2007 Jul;293(1):E16-23.

Protocol

Cell experiment [1]:
Cell lines	ECSCs and NESCs
Preparation method	The solubility of this compound in DMSO is > 12.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.
Reacting condition	0.01 ~ 10 μM;
Applications	In ECSCs and NESCs, BAY 11-7085 significantly inhibited cell viability in a dose-dependent manner. At the dose of 10 μM, ECSCs and NESCs treated with BAY 11-7085 showed 66.1% and 54.7% decreases in cell viability, respectively. In addition, according to the results of the BrdU incorporation assay, at the dose of 10 μM, BAY 11-7085 significantly inhibited the BrdU incorporation of ECSCs in a dose-dependent manner (53.2% decrease), whereas BAY 11-7085 only showed a weak inhibitory effect on the BrdU incorporation of NESCs (38.2% decrease). Therefore, BAY 11-7085 showed stronger inhibitory effects on the cell viability and the cell proliferation of ECSCs than on those of NESCs.
Animal experiment [2]:
Animal models	Rat model of pneumococcal meningitis
Dosage form	20 mg; i.p.
Applications	In rat model of pneumococcal meningitis, BAY 11-7085 significantly reduced meningitis-associated loss of cerebrovascular autoregulation. Besides, also BAY 11-7085 also significantly reduced increases in CSF WBCs, ICP and BBB permeability caused by pneumococcal infection. The results of Western blot analysis showed BAY 11-7085 inhibited meningitis-associated increase in NF-κB activity.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
参考文献: [1]. Nasu K1, Nishida M, Ueda T, Yuge A, Takai N, Narahara H. Application of the nuclear factor-kappaB inhibitor BAY 11-7085 for the treatment of endometriosis: an in vitro study. Am J Physiol Endocrinol Metab. 2007 Jul;293(1):E16-23 [2]. Koedel U, Bayerlein I, Paul R, Sporer B, Pfister HW. Pharmacologic interference with NF-kappaB activation attenuates central nervous system complications in experimental Pneumococcal meningitis. J Infect Dis. 2000 Nov;182(5):1437-45.