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Bay 11-7821 (BAY 11-7082) BAY 11-7821

BAY 11-7082 (BAY 11-7821)是一种 NF-κB 抑制剂,抑制TNFα诱导的 IκBα 磷酸化,在肿瘤细胞中IC50为10 μM。BAY 11-7082 可抑制 ubiquitin-specific protease USP7 和 USP21,对应的IC50值分别为0.19 μM和0.96 μM。BAY 11-7082 在胃癌细胞中可诱导凋亡和S期阻滞。

  • 货号:
    TK0198
  • 规格:
    1mg
    5mg
    10mg
    25mg
  • 价格:
    0.00

产品参数

CAS No.19542-67-7
生物活性BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
分子式C10H9NO2S
分子量207.25
储存条件Powder -20℃ 3 years
溶解性数据DMSO : ≥ 100 mg/mL (482.51 mM)
体内研究BAY 11-7082 (2.5 mg/kg and 5 mg/kg; intratumoral injection; twice-weekly for 21 days ) significantly suppresses tumor growth in a dose-dependent manner.
体外研究BAY 11-7082 (BAY 11-7821), an inhibitor of NF-κB, induces apoptosis of HTLV-I-infected T-cell lines but only negligible apoptosis of HTLV-I-negative T cells. Bay 11-7082 rapidly and efficiently reduces the DNA binding of NF-κB in HTLV-I-infected T-cell lines and down-regulated 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 inhibits NFκB signalling and is recently shown to inhibit the majority of E2 and E3 ligases tested by reacting covalently with the catalytic cysteine residues. Moreover, BAY 11-7082 also inhibits several tyrosine phosphatases by reacting with catalytic Cys residue of these enzymes. NSC 697923 is originally shown to inhibit the E2 ligase Ubc13-Uev1A. BAY 11-7082 inhibits the phosphorylation of IκBα and activation of NF-κB, induces the death of HBL-1 cells. BAY 11-7082 completely suppresses the LPS-stimulated and IL-1-stimulated phosphorylation of the activation loop of IKKβ. BAY 11-7082 acts by inhibiting TNF-α-induced phosphorylation of IκB-α, resulting in decreased NF-κB and decreases expression of adhesion molecules.
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纯度及产品资料98%