BAY 11-7082; BAY 11-7821 [T1902][CAS no. 19542-67-7]_TargetMol - 코아사이언스

안녕하세요!

TargetMol (Target molecule Corp.) 공식 수입/공급 업체 코아사이언스 입니다.

 

자세한 상품 정보 및 관련 문의는 전화 02-858-0328 또는 info@coresciences.co.kr로 문의주시기 바랍니다.

감사합니다!

 

BAY 11-7082

=BAY 11-7821

Cat.# T1902 / Size: 5mg, 10mg, 25mg, 50mg, 100mg, 200mg, 500mg

Biological Description

Description	BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that inhibits TNFα-induced IκBα phosphorylation (IC50=10 μM). BAY 11-7082 is also an inhibitor of the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19/0.96 μM).
Targets&IC50	IκBα phosphorylation:10 μM
In vitro	METHODS: Human colorectal cancer cells HT29 were treated with BAY 11-7082 (10-100 µM) for 1 h, followed by stimulation with TNF (50 ng/mL) for 3-10 min or Flag-TWEAK (200 ng/mL) for 8 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Bay 11-7082 inhibited TWEAK-induced p100 processing and TNF-induced phosphorylation and degradation of IκBα. Both NFκB pathways were significantly blocked at concentrations of 30-100 µM of Bay 11-7082. [1] METHODS: Macrophage RAW264.7 was treated with BAY 11-7082 (15 µM) and LPS (1 µg/mL) for 6 h, and TNF-α levels were measured by ELISA Assay. RESULTS: BAY 11-7082 blocked TNF-α production in LPS-treated RAW264.7 cells, which is an inflammatory response generated by activated NF-κB. [2]
In vivo	METHODS: To investigate the immunomodulatory effects, BAY 11-7082 (5-10 mg/kg) was injected intraperitoneally into C57BL/6 mice, followed 1 h later by intravenous injection of poly U (50 µg/head) + in vivo-jetPEI. RESULTS: Treatment with BAY 11-7082 inhibits the IFN response in vivo by limiting pDC function when stimulated with TLR ligands. [3] METHODS: To investigate the effects on psoriasiform dermatitis, BAY 11-7082 (20 mg/kg) was injected intraperitoneally into C57BL/6 and NLRP3 KO mice with IMQ-induced psoriasiform lesions once daily for seven days. RESULTS: BAY 11-7082 blunted epidermal thickness, acanthosis and inflammatory infiltrates.BAY 11-7082 decreased the expression of pNF-κB, NLRP3, TNF-α, IL-6 and IL-1β, attenuated the phosphorylation of signal transducers and STAT3, and lowered IL-23 levels. [4]
Kinase Assay	UBE1 (0.17 μM) in 22.5 μL of 20 mM Hepes, pH 7.5, containing 10 μM ubiquitin is incubated for 45 min at 21°C with 1 μL of DMSO or 1 μL of BAY 11-7082 in DMSO. A 2.5 μL solution of 10 mM magnesium acetate and 0.2 mM ATP is added, incubated for 10 min at 30°C, and the reactions are terminated by the addition of 2.5 μL of 10% (w/v) SDS and heating for 6 min at 75°C. The samples are subjected to SDS/PAGE in the absence of any thiol. The gels are stained for 1 h with Coomassie Instant Blue and destained by washing with water. The loading of ubiquitin to E2 conjugating enzymes is carried out in an identical manner, except that UBE1 (0.17 μM) is mixed with Ubc13 (2.4 μM) or UbcH7 (2.9 μM) prior to incubation with BAY 11-7082[3].
Cell Research	Cells are transfected with siRNA in 96-well microtiter plates and then cultured for 72 hours in complete NSCLC medium, treated with BAY 11-7082 for 12 hours. Cells are incubated with [3H]thymidine for 3 hours. The cells are collected on filters using an automatic cell harvester and radioactivity on the filters is measured by β-scintillation counting.(Only for Reference)

Chemical Properties

Synonyms	BAY 11-7821
Molecular Weight	207.25
Formula	C10H9NO2S
CAS No.	19542-67-7

References and Literature

1. Rauert-Wunderlich H, et al. The IKK inhibitor Bay 11-7082 induces cell death independent from inhibition of activation of NFκB transcription factors. PLoS One. 2013;8(3):e59292.

2. Lee J, et al. BAY 11-7082 is a broad-spectrum inhibitor with anti-inflammatory activity against multiple targets. Mediators Inflamm. 2012;2012:416036.

3. Miyamoto R, et al. Inhibitor of IkappaB kinase activity, BAY 11-7082, interferes with interferon regulatory factor 7 nuclear translocation and type I interferon production by plasmacytoid dendritic cells. Arthritis Res Ther. 2010;12(3):R87.

4. Irrera N, et al. BAY 11-7082 inhibits the NF-κB and NLRP3 inflammasome pathways and protects against IMQ-induced psoriasis. Clin Sci (Lond). 2017 Mar 1;131(6):487-498.

5. Goffi F, et al. Neurosci Lett, 2005, 377(3), 147-151.

6. Jun Jacob Hu, et al. Identification of pyroptosis inhibitors that target a reactive cysteine in gasdermin D. The Preprint Server For Biology, 2018,Jul. 10.

7. Shen S C, He F, Cheng C, et al. Uric acid aggravates myocardial ischemia–reperfusion injury via ROS/NLRP3 pyroptosis pathway[J]. Biomedicine & Pharmacotherapy . 2020, 133: 110990.

8. Yu Y, Li Z, Guo R, et al. Ononin, sec-O-β-D-glucosylhamaudol and astragaloside I: antiviral lead compounds identified via high throughput screening and biological validation from traditional Chinese medicine Zhongjing formulary[J]. Pharmacological Research. 2019 May 11;145:104248.

10. Gao J, Wang Y, Zhang W, et al. C20orf27 Promotes Cell Growth and Proliferation of Colorectal Cancer via the TGFβR-TAK1-NFĸB Pathway[J]. Cancers. 2020, 12(2): 336.

​

Citations

1. Ye Z, Ai X, Yang K, et al.Targeting Microglial Metabolic Rewiring Synergizes with Immune Checkpoint Blockade Therapy for Glioblastoma.Cancer Discovery.2023

2. Jiang Y, Zhao X, Chen J, et al.PM2. 5 induces cardiac malformations via PI3K/akt2/mTORC1 signaling pathway in zebrafish larvae.Environmental Pollution.2023: 121306.

3. Yu D, Cai W, Shen T, et al.PM2. 5 exposure increases dry eye disease risks through corneal epithelial inflammation and mitochondrial dysfunctions.Cell Biology and Toxicology.2023: 1-16.

4. Tang S, Zhong W, Li T, et al.Isochlorogenic acid A alleviates dextran sulfate sodium-induced ulcerative colitis in mice through STAT3/NF-кB pathway.International Immunopharmacology.2023, 118: 109989.

5. Gao J, Wang Y, Zhang W, et al. C20orf27 Promotes Cell Growth and Proliferation of Colorectal Cancer via the TGFβR-TAK1-NFĸB Pathway. Cancers. 2020, 12(2): 336

6. Yu Y, Li Z, Guo R, et al. Ononin, sec-O-β-D-glucosylhamaudol and astragaloside I: antiviral lead compounds identified via high throughput screening and biological validation from traditional Chinese medicine Zhongjing formulary. Pharmacological Research. 2019 May 11;145:104248

7. Chen H, He A, Li H, et al. TSSK4 upregulation in alveolar epithelial type-II cells facilitates pulmonary fibrosis through HSP90-AKT signaling restriction and AT-II apoptosis. Cell Death & Disease. 2021, 12(10): 1-1

8. Shen S C, He F, Cheng C, et al. Uric acid aggravates myocardial ischemia–reperfusion injury via ROS/NLRP3 pyroptosis pathway. Biomedicine & Pharmacotherapy. 2020, 133: 110990.

9. Du T, Yan Z, Zhu S, et al. QKI deficiency leads to osteoporosis by promoting RANKL-inducedosteoclastogenesis and disrupting bone metabolism. Cell Death and Disease. 2020

10. Du T, Yan Z, Zhu S, et al. QKI deficiency leads to osteoporosis by promoting RANKL-inducedosteoclastogenesis and disrupting bone metabolism. Cell Death and Disease. 2020

​

* 본 상품은 오직 연구용으로만 사용 가능합니다. 인체 및 제품화에 사용하실 수 없습니다.

코아사이언스 coresciences Target molecule Corp TargetMol USA distributor Korea 한국 대리점