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首页-小分子抑制剂&激动剂-NF-κB Pathway-NF-κB-BAY 11-7082
BAY 11-7082

Chemical Structure : BAY 11-7082

CAS No.: 19542-67-7

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BAY 11-7082 (BAY 117821)

货号: PC-43543Not For Human Use, Lab Use Only.

BAY 11-7082 is a NF-κB inhibitor that selectively and irreversibly inhibits the TNF-α-inducible phosphorylation of IκBα (IC50=10 uM), also inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 uM and 0.96 uM, respectively.

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50 mg ￥1480 In stock
100 mg ￥2580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BAY 11-7082 is a NF-κB inhibitor that selectively and irreversibly inhibits the TNF-α-inducible phosphorylation of IκBα (IC50=10 uM), also inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 uM and 0.96 uM, respectively.
BAY 11-7082 induces apoptosis of HTLV-I-infected T-cell lines but only negligible apoptosis of HTLV-I-negative T cells, rapidly and efficiently reduces the DNA binding of NF-κB in HTLV-I-infected T-cell lines and down-regulates the expression of the antiapoptotic gene, Bcl-xL, regulated by NF-κB.
BAY 11-7082 selectively inhibits Tax-induced NF-κB activity in a human T-cell line.
BAY 11-7082 exerts effects by inactivating the E2-conjugating enzymes Ubc (ubiquitin conjugating) 13 and UbcH7 and the E3 ligase LUBAC (linear ubiquitin assembly complex), thereby preventing the formation of Lys63-linked and linear polyubiquitin chains.
BAY 11-7082 prevents ubiquitin conjugation to Ubc13 and UbcH7 by forming a covalent adduct with their reactive cysteine residues.

物理化学性质&存储条件

分子量 207.249
分子式 C10H9NO2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-Propenenitrile, 3-[(4-methylphenyl)sulfonyl]-, (2E)-

参考文献

1. Thévenod F, et al. J Biol Chem. 2000 Jan 21;275(3):1887-96.
2. Mori N, et al. Blood. 2002 Sep 1;100(5):1828-34.
3. Ritorto MS, et al. Nat Commun. 2014 Aug 27;5:4763.
4. Strickson S, et al. Biochem J. 2013 May 1;451(3):427-37.

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