Bay 11-7821 (Synonyms: BAY 11-7082) |
| Catalog No.GC13035 |
Bay 11-7821(BAY 11-7082) is an inhibitor of IκBα phosphorylation and NF-κB, selectively and irreversibly inhibits TNF-α-induced IκB-α phosphorylation (IC50 value is approximately 10μM), and reduces the expression of NF-κB and adhesion molecules. Bay 11-7821 inhibits ubiquitin-specific proteases USP7 and USP21 with IC50 values of 0.19 and 0.96μM, respectively .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 19542-67-7
Sample solution is provided at 25 µL, 10mM.
Bay 11-7821(BAY 11-7082) is an inhibitor of IκBα phosphorylation and NF-κB, selectively and irreversibly inhibits TNF-α-induced IκB-α phosphorylation (IC50 value is approximately 10μM), and reduces the expression of NF-κB and adhesion molecules [1]. Bay 11-7821 inhibits ubiquitin-specific proteases USP7 and USP21 with IC50 values of 0.19 and 0.96μM, respectively [2]. Bay 11-7821 inhibits the formation of pores in liposomes by the pore-forming protein gasdermin D (GSDMD), as well as inflammasome-mediated apoptosis and IL-1β secretion [3].
In vitro, Bay 11-7821 (0-30μM) treated gastric cancer cells (HGC-27, NCI-N87, AGS and MGC80-3) for 24h, inhibited cell viability in a dose-dependent manner, Bcl-2 (total and phosphorylated forms) were significantly downregulated, while Bax was upregulated, and induced S phase arrest by inhibiting cyclin A and CDK-2 expression [4]. Bay 11-7821 (3μM) treated HBL-1 cells for 24-72h, inhibited IκB-α phosphorylation and NF-κB activation, and induced cell death [5]. Bay 11-7821 (30μM) treated KMS-12-BM and MM.1S MM cells rapidly induced cell death, with decreased viability detected within 1h, and complete inhibition of cell viability was achieved within 2-4 hours [6].
In vivo, intraperitoneal injection of Bay 11-7821 (1, 3 mg/kg) in diabetic rats with renal dysfunction significantly improved the decreased levels of SOD and GSH, as well as the increased levels of lipid peroxidation and nitric oxide, and restored the renal histological structure of diabetic rats [7].
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] Ritorto M S, Ewan R, Perez-Oliva A B, et al. Screening of DUB activity and specificity by MALDI-TOF mass spectrometry[J]. Nature communications, 2014, 5(1): 4763.
[3] Hu J J, Liu X, Zhao J, et al. Identification of pyroptosis inhibitors that target a reactive cysteine in gasdermin D[J]. BioRxiv, 2018: 365908.
[4] Chen L, Ruan Y, Wang X, et al. BAY 11-7082, a nuclear factor-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells[J]. Journal of gastroenterology, 2014, 49: 864-874.
[5] Strickson S, Campbell D G, Emmerich C H, et al. The anti-inflammatory drug BAY 11-7082 suppresses the MyD88-dependent signalling network by targeting the ubiquitin system[J]. Biochemical Journal, 2013, 451(3): 427-437.
[6] Rauert-Wunderlich H, Siegmund D, Maier E, et al. The IKK inhibitor Bay 11-7082 induces cell death independent from inhibition of activation of NFκB transcription factors[J]. PloS one, 2013, 8(3): e59292.
[7] Kolati S R, Kasala E R, Bodduluru L N, et al. BAY 11-7082 ameliorates diabetic nephropathy by attenuating hyperglycemia-mediated oxidative stress and renal inflammation via NF-κB pathway[J]. Environmental Toxicology and Pharmacology, 2015, 39(2): 690-699.
| Cell experiment [1]: | |
Cell lines | HGC-27、NCI-N87、AGS、MGC80-3 cells |
Preparation Method | Cells were treated with Bay 11-7821 (0-30μM), and cell viabilities were detected at 6 and 24 h. |
Reaction Conditions | 0-30μM; 6、24h |
Applications | BAY 11-7082 inhibited cell viability in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Rats were treated with Bay 11-7821 (1mg/kg and 3mg/kg) intraperitoneally after STZ injection and for the next 4 weeks. |
Dosage form | 1、3mg/kg; i.p. |
Applications | Bay 11-7821-treated rats showed significant improvements in the levels of the enzymatic antioxidant SOD, the non-enzymatic antioxidant GSH, and the increased levels of lipid peroxidation and nitric oxide. Bay 11-7821 treatment significantly restored the renal histological structure of diabetic rats. |
References: [1] Chen L, Ruan Y, Wang X, et al. BAY 11-7082, a nuclear factor-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells[J]. Journal of gastroenterology, 2014, 49: 864-874. [2] Kolati S R, Kasala E R, Bodduluru L N, et al. BAY 11-7082 ameliorates diabetic nephropathy by attenuating hyperglycemia-mediated oxidative stress and renal inflammation via NF-κB pathway[J]. Environmental Toxicology and Pharmacology, 2015, 39(2): 690-699. | |
| Cas No. | 19542-67-7 | SDF | |
| Synonyms | BAY 11-7082 | ||
| Chemical Name | (E)-3-(4-methylphenyl)sulfonylprop-2-enenitrile | ||
| Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)C=CC#N | ||
| Formula | C10H9NO2S | M.Wt | 207.25 |
| Solubility | ≥ 64 mg/mL in DMSO, ≥ 10.64 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.8251 mL | 24.1255 mL | 48.2509 mL |
| 5 mM | 0.965 mL | 4.8251 mL | 9.6502 mL |
| 10 mM | 0.4825 mL | 2.4125 mL | 4.8251 mL |
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Quality Control & SDS
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- Purity: >99.50%
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Related Biological Data
Concentrations of IL-8, IL-1β and TNF-α in supernatants of IPEC-J2 cells. IPEC-J2 cells added with DMSO were regarded as the vehicle control and L. salivarius-involved IPEC-J2 cells were supplemented with (a) 10 μmol/L SB-203580, (b) 10 μmol/L SCH772984 and (c) 10 μmol/L BAY11-7082, respectively.
BAY11–7082 (GlpBio) were first employed in IPEC-J2 cells for 1 h [19–21], followed by L. salivarius involvement for 3 h. After 3 times washes with PBS, IPEC-J2 cells were infected with ETEC K88 for 3, 6, 12 and 24h,respectively.
J Anim Sci Biotechno 11.1 (2020): 1-13. PMID: 32774852 IF: 5.034 -
Related Biological Data
Effects of AFR on the expression of the BDNF-MEK/ERK signalling pathway in the hippocampus (D) Effects of AZD6244 and BAY11-7082 inhibitors on cell viability after AFR treatment and CORT induction.
In vitro, HT-22 cells were treated with corticosterone (CORT) solution (0.35 mg/mL), then AFR (0.05mg/mL) solution and inhibitor AZD6244 (14 μM/mL) or BAY11-7082 (10 μM/mL) (GlpBio) were added, respectively.
Pharmaceutical Biology 60.1 (2022): 1436-1448. PMID: 35938494 IF: 3.8892
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