BAY 11-7082

• CAT Number: I002493
• CAS Number: 19542-67-7
• Molecular Formula: C10H9NO2S
• Molecular Weight: 207.247
• Purity: ≥95%
• Target: IκB/IKK
• Solubility: 10 mM in DMSO
• Storage: 3 years -20C powder
• IC50: 10 μM
• IUPAC Name: (E)-3-(4-methylphenyl)sulfonylprop-2-enenitrile
• InChI: InChI=1S/C10H9NO2S/c1-9-3-5-10(6-4-9)14(12,13)8-2-7-11/h2-6,8H,1H3/b8-2+
• InChIKey: DOEWDSDBFRHVAP-KRXBUXKQSA-N
• SMILES: CC1=CC=C(C=C1)S(=O)(=O)C=CC#N

BAY 11-7082 (CAT: I002493) serves as an irreversible inhibitor of IKKα, impeding phosphorylation of cytokine-inducible IκBα (nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor-α) with an IC50 of 10 μM. This compound’s actions extend to NF-κB modulation, inducing apoptosis in HTLV-I-infected T-cell lines and adult T-cell leukemia cells by down-regulating the antiapoptotic gene Bcl-xL governed by NF-κB. Additionally, BAY 11-7082 inhibits ubiquitin loading onto E2 conjugating enzymes, demonstrating poor selectivity for IKK1 and IKK2. 

Reference

1:BAY 11-7082 inhibits the NF-κB and NLRP3 inflammasome pathways and protects against IMQ-induced psoriasis. Irrera N, Vaccaro M, Bitto A, Pallio G, Pizzino G, Lentini M, Arcoraci V, Minutoli L, Scuruchi M, Cutroneo G, Anastasi GP, Ettari R, Squadrito F, Altavilla D.Clin Sci (Lond). 2017 Mar 1;131(6):487-498. doi: 10.1042/CS20160645. Epub 2017 Jan 17. PMID: 28096316 2:Pharmacological targeting of glucose-6-phosphate dehydrogenase in human erythrocytes by Bay 11-7082, parthenolide and dimethyl fumarate. Ghashghaeinia M, Giustarini D, Koralkova P, Köberle M, Alzoubi K, Bissinger R, Hosseinzadeh Z, Dreischer P, Bernhardt I, Lang F, Toulany M, Wieder T, Mojzikova R, Rossi R, Mrowietz U.Sci Rep. 2016 Jun 29;6:28754. doi: 10.1038/srep28754. PMID: 27353740 Free PMC Article3:BAY 11-7082 ameliorates diabetic nephropathy by attenuating hyperglycemia-mediated oxidative stress and renal inflammation via NF-κB pathway. Kolati SR, Kasala ER, Bodduluru LN, Mahareddy JR, Uppulapu SK, Gogoi R, Barua CC, Lahkar M.Environ Toxicol Pharmacol. 2015 Mar;39(2):690-9. doi: 10.1016/j.etap.2015.01.019. Epub 2015 Feb 7. PMID: 25704036 4:Nuclear factor κB inhibitor BAY 11-7082 suppresses oxidative stress induced by endothelin-1 (ET-1) in rat kidney. Kowalczyk A, Kołodziejczyk M, Gorąca A.Postepy Hig Med Dosw (Online). 2015 Dec 31;69:1512-8. PMID: 27259223 Free Article5:BAY 11-7082, a nuclear factor-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells. Chen L, Ruan Y, Wang X, Min L, Shen Z, Sun Y, Qin X.J Gastroenterol. 2014 May;49(5):864-74. doi: 10.1007/s00535-013-0848-4. Epub 2013 Jul 12. PMID: 23846545 6:The anti-inflammatory compound BAY-11-7082 is a potent inhibitor of protein tyrosine phosphatases. Krishnan N, Bencze G, Cohen P, Tonks NK.FEBS J. 2013 Jun;280(12):2830-41. doi: 10.1111/febs.12283. Epub 2013 May 9. PMID: 23578302 Free PMC Article7:The IKK inhibitor Bay 11-7082 induces cell death independent from inhibition of activation of NFκB transcription factors. Rauert-Wunderlich H, Siegmund D, Maier E, Giner T, Bargou RC, Wajant H, Stühmer T.PLoS One. 2013;8(3):e59292. doi: 10.1371/journal.pone.0059292. Epub 2013 Mar 20. PMID: 23527154 Free PMC Article8:The anti-inflammatory drug BAY 11-7082 suppresses the MyD88-dependent signalling network by targeting the ubiquitin system. Strickson S, Campbell DG, Emmerich CH, Knebel A, Plater L, Ritorto MS, Shpiro N, Cohen P.Biochem J. 2013 May 1;451(3):427-37. doi: 10.1042/BJ20121651. PMID: 23441730 Free PMC Article9:BAY 11-7082 is a broad-spectrum inhibitor with anti-inflammatory activity against multiple targets. Lee J, Rhee MH, Kim E, Cho JY.Mediators Inflamm. 2012;2012:416036. doi: 10.1155/2012/416036. Epub 2012 Jun 15. PMID: 22745523 Free PMC Article10:Alpha-tocopherol and BAY 11-7082 reduce vascular cell adhesion molecule in human aortic endothelial cells. Catalán U, Fernández-Castillejo S, Pons L, Heras M, Aragonés G, Anglès N, Morelló JR, Solà R.J Vasc Res. 2012;49(4):319-28. doi: 10.1159/000337466. Epub 2012 May 9. PMID: 22572606