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Submit ReviewBay 11-7821 is an E2 ubiquitin (Ub) conjugating enzyme inhibitor. Inhibits the conjugation of Ub to a range of E2 enzymes. Inhibits E2 enzyme mediated IκBα phosphorylation and indirectly decreases NF-κb activity. Also reversibly activates MAPK signaling. Induces apoptosis of leukemic T cell and B-cell lymphoma cell lines. Also inhibits activation of NLRP3 inflammasome. Binds and inhibits gasdermin D (GSDMD) pore formation. Pyroptosis inhibitor.
分子量 | 207.25 |
公式 | C10H9NO2S |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 19542-67-7 |
PubChem ID | 5353431 |
InChI Key | DOEWDSDBFRHVAP-KRXBUXKQSA-N |
Smiles | CC1=CC=C(C=C1)S(=O)(=O)\C=C\C#N |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
ethanol | 5.18 | 25 | |
DMSO | 20.73 | 100 |
以下数据基于产品分子量 207.25。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 4.83 mL | 24.13 mL | 48.25 mL |
5 mM | 0.97 mL | 4.83 mL | 9.65 mL |
10 mM | 0.48 mL | 2.41 mL | 4.83 mL |
50 mM | 0.1 mL | 0.48 mL | 0.97 mL |
参考文献是支持产品生物活性的出版物。
Mori et al (2002) Bay 11-7082 inhibits transcription factor NF-κB and induces apoptosis of HTLV-I-infected T-cell lines and primary adult T-cell leukemia cells. Blood 100 1828 PMID: 12176906
Pierce et al (1997) Novel inhibitors of cytokine-induced IκBα phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo. J.Biol.Chem. 272 21096 PMID: 9261113
Strickson et al (2013) The anti-inflammatory drug BAY 11-7082 suppresses the MyD88-dependent signalling network by targeting the ubiquitin system. Biochem.J. 451 427 PMID: 23441730
Juliana et al (2010) Anti-inflammatory compounds parthenolide and Bay 11-7082 are direct inhibitors of the inflammasome. J.Biol.Chem. 285 9792 PMID: 20093358
Pandeya et al (2019) Gasdermin D (GSDMD) as a new target for the treatment of infection. Medchemcomm 10 660 PMID: 31191857
If you know of a relevant reference for Bay 11-7821, please let us know.
关键词: Bay 11-7821, Bay 11-7821 supplier, Irreversible, inhibitors, inhibits, TNF-α, TNF-alpha-induced, IκB, IκBα, IkappaBalpha, phosphorylation, IkappaB, Nuclear, Factor, Kappa, B, NF-κB, NF-kappaB, and, Cytokine, Signaling, Signalling, Transcription, Factors, Bay11-7821, Bay117082, NF-kB, NLRP3, Bay, 11-7082, NF-kB/IkB, Post-translational, Modifications, Ubiquitin/Ubl, E2, Conjugating, Enzymes, Inflammasomes, 1744, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Bay 11-7821 的部分引用包括:
Zhou (2017) TNFα induces tolerant production of CXC chemokines in colorectal cancer HCT116 cells via A20 inhibition of ERK signaling. Int Immunopharmacol 54 296 PMID: 29175508
Clement et al (2014) CD31 is a key coinhibitory receptor in the development of immunogenic dendritic cells. Proc Natl Acad Sci U S A 111 E1101 PMID: 24616502
Jiang (2017) Targeting the NLRP3 inflammasome to attenuate spinal cord injury in mice. J Neuroinflammation 14 207 PMID: 29070054
Han et al (2017) Nonsaponin fractions of Korean Red Ginseng extracts prime activation of NLRP3 inflammasome. J Ginseng Res 41 513 PMID: 29021698
Yu et al (2014) Differential effects of the Toll-like receptor 2 agonists, PGN and Pam3CSK4 on anti-IgE induced human mast cell activation. PLoS One 9 e112989 PMID: 25398056
Ahn et al (2019) Nonsaponin fraction of Korean Red Ginseng attenuates cytokine production via inhibition of TLR4 expression. J Ginseng Res 43 291 PMID: 30976167
Jia et al (2015) β-Catenin and NF-κB co-activation triggered by TLR3 stimulation facilitates stem cell-like phenotypes in breast cancer. Cell Death Differ 22 298 PMID: 25257174
Yang et al (2011) Constitutive NF-kappaB activation confers interleukin 6 (IL6) independence and resistance to dexameth. and Janus kinase inhibitor INCB018424 in murine plasmacytoma cells. J Biol Chem 286 27988 PMID: 21705340
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