Bay 11-7085是一种NF-κB活化和IκBα磷酸化的抑制剂，对IκBα的IC50值为10μM。
Cas No.:196309-76-9
Sample solution is provided at 25 µL, 10mM.
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Bay 11-7085 is an inhibitor of NF-κB activation and phosphorylation of IκBα with an IC50 value of 10μM for IκBα[1]. Bay 11-7085 inactivates protein tyrosine phosphatases (PTPs) by forming a covalent adduct with the active-site cysteine and inhibits the signal-induced nuclear translocation of NFκB through inhibiting IKK activity and the phosphorylation of IκB in response to the signal [2]. Bay 11-7085 has been widely used to inhibit and eradicate the formation of biofilms by various pathogens, and to prevent the growth of various pathogenic microorganisms[3].
In vitro, Bay 11-7085 treatment for 24 hours significantly inhibited the viability of Nalm6 cells and Raji cells, with IC50 values of 0.5μM and 3.1μM, respectively[4]. Treatment with 10μM Bay 11-7085 for 2 hours induces an increase in LC3B-II in human synovial fibroblasts, phosphorylation of the glucocorticoid receptor (GR) at serine 211, and promotes autophagy of the cells[5]. Treatment with 4μM Bay 11-7085 for 24 hours promoted apoptosis in L1210 cells, accompanied by an increase in caspase-3 activity[6].
In vivo, Bay 11-7085 treatment via intraperitoneal injection (5mg/kg) every three days for a total of 9 days significantly reduced the tumor burden in the Su.86 xenograft mouse model [7]. Weekly intraperitoneal injection of Bay 11-7085 (5mg/kg) twice for 28 days significantly reduced the tumor volume and liver metastasis in the HT-29 xenograft mouse model[8].
References:
[1] Pierce J W, Schoenleber R, Jesmok G, et al. Novel inhibitors of cytokine-induced IκBα phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo[J]. Journal of Biological Chemistry, 1997, 272(34): 21096-21103.
[2] Krishnan N, Bencze G, Cohen P, et al. The anti‐inflammatory compound BAY‐11‐7082 is a potent inhibitor of protein tyrosine phosphatases[J]. The FEBS journal, 2013, 280(12): 2830-2841.
[3] Escobar I E, Possamai Rossatto F C, Kim S M, et al. Repurposing kinase Inhibitor Bay 11-7085 to combat Staphylococcus aureus and Candida albicans biofilms[J]. Frontiers in Pharmacology, 2021, 12: 675300.
[4] Berger N, Bassat H B, Klein B Y, et al. Cytotoxicity of NF-κB inhibitors Bay 11-7085 and caffeic acid phenethyl ester to Ramos and other human B-lymphoma cell lines[J]. Experimental hematology, 2007, 35(10): 1495-1509.
[5] Relic B, Charlier E, Deroyer C, et al. BAY 11-7085 induces glucocorticoid receptor activation and autophagy that collaborate with apoptosis to induce human synovial fibroblast cell death[J]. Oncotarget, 2016, 7(17): 23370.
[6] Cory A H, Cory J G. Induction of apoptosis in p53-deficient L1210 cells by an I-κ-B-α-inhibitor (Bay 11-7085) via a NF-κ-B-independent mechanism[J]. Advances in enzyme regulation, 2005, 45(1): 85-93.
[7] Shen Y, Herde R, Doxey B W, et al. Pharmacologic downregulation of c‐FLIPL restores juxtacrine death receptor‐mediated apoptosis in cancer cells in a peritoneal carcinomatosis model[J]. International journal of cancer, 2012, 130(7): 1494-1503.
[8] Scaife C L, Kuang J, Wills J C, et al. Nuclear factor κB inhibitors induce adhesion-dependent colon cancer apoptosis: implications for metastasis[J]. Cancer research, 2002, 62(23): 6870-6878.
Bay 11-7085是一种NF-κB活化和IκBα磷酸化的抑制剂，对IκBα的IC50值为10μM [1]。Bay 11-7085通过与活性位点半胱氨酸形成共价加合物来灭活蛋白酪氨酸磷酸酶(PTPs)，并通过抑制IKK活性以及响应信号时IκB的磷酸化来抑制信号诱导的NFκB核转位[2]。Bay 11-7085已被广泛用于抑制和根除多种病原体形成的生物膜，并预防多种病原微生物的生长[3]。
在体外，Bay 11-7085处理24小时显著抑制了Nalm6细胞和Raji细胞的活力，IC50值分别为0.5μM和3.1μM[4]。10μM的Bay 11-7085处理人滑膜成纤维细胞2小时，可诱导LC3B-II增加、糖皮质激素受体(GR)在丝氨酸211位点磷酸化，并促进细胞自噬[5]。4μM的Bay 11-7085处理L1210细胞24小时，促进了细胞凋亡，同时伴随caspase-3活性升高[6]。
在体内，每隔三天腹腔注射5mg/kg剂量的Bay 11-7085，共9天，显著降低了Su.86异种移植小鼠模型中的肿瘤负荷[7]。每周腹腔注射5mg/kg的Bay 11-7085两次，持续28天，显著降低了HT-29异种移植小鼠模型中的肿瘤体积和肝转移[8]。
| Cell experiment [1]: | |
Cell lines | Ramos B-lymphoma cells |
Preparation Method | Ramos B-lymphoma cells were grown in RPMI-1640 medium with 10% (v/v) fetal bovine serum (FBS), 0.2mM glutamine, 100U/ml penicillin, and 100μg/ml streptomycin at 37°C in 5% CO2/atmosphere. Cells (2×105 cells/ml) were seeded onto 24-well plates and allowed to adhere in a 5% CO2 incubator at 37°C overnight. Cells were treated with different concentrations of Bay 11-7085 (0, 2, 4, 6, 8, and 10µM) for 24h. Control cells were treated with DMSO at a final concentration of 0.1%. Cell viability was evaluated. |
Reaction Conditions | 0, 2, 4, 6, 8, and 10µM; 24h |
Applications | Bay 11-7085 treatment significantly reduced the cell viability of Ramos B-lymphoma cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female nu/nu athymic mice |
Preparation Method | Female nu/nu athymic mice (5 weeks old) were housed singly in a standard environment with food and water ad libitum. HT-29 cells were harvested in 0.25% trypsin-PBS-EDTA, washed once each in medium and PBS, and resuspended in PBS at 1×107 cells/200μl. 1×107 HT-29 cells were injected either s.c. in the backs or i.p. in 5-week-old female nu/nu athymic mice. For the mice with s.c. tumors, the tumors were allowed to establish themselves for 10 days after which the mice were randomized to BAY 11-7085 or DMSO. All of the mice received BAY 11-7085 (5mg/kg) or an equal volume of DMSO (200μl) twice weekly for 28 days. Tumor size was determined by measuring the length and width with calipers. |
Dosage form | 5mg/kg; twice a week for 28 days; i.p. |
Applications | BAY 11-7085 treatment significantly reduced the tumor volume in the HT-29 xenograft mouse model. |
References: | |
| Cas No. | 196309-76-9 | SDF | |
| 别名 | (2E)-3-[[4-叔丁基苯基]磺酰基]-2-丙烯腈,BAY 11-7083 | ||
| 化学名 | (E)-3-(4-tert-butylphenyl)sulfonylprop-2-enenitrile | ||
| Canonical SMILES | CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)C=CC#N | ||
| 分子式 | C13H15NO2S | 分子量 | 249.33 |
| 溶解度 | ≥ 12.45mg/mL in DMSO | 储存条件 | Store at -20° C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0107 mL | 20.0537 mL | 40.1075 mL |
| 5 mM | 802.1 μL | 4.0107 mL | 8.0215 mL |
| 10 mM | 401.1 μL | 2.0054 mL | 4.0107 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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