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CAS No. : 19542-67-7
MCE 国际站:BAY 11-7082
产品活性:BAY 11-7082 (BAY 11-7821) 是一种 IκBα 磷酸化和 NF-κB 抑制剂,选择性且不可逆地抑制 TNF-α 诱导的 IκB-α 磷酸化,并减少 NF-κB 和粘附分子的表达。BAY 11-7082 抑制泛素特异性蛋白酶 USP7 和 USP21 (IC50分别为 0.19, 0.96 μM)。BAY 11-7082 抑制脂质体中的 gasdermin D (GSDMD) 孔形成以及炎性体介导的细胞凋亡和人和小鼠细胞中IL-1β的分泌。
研究领域:NF-κB | Cell Cycle/DNA Damage | Autophagy | Apoptosis
作用靶点:IKK | Deubiquitinase | Autophagy | Apoptosis | NF-κB
In Vitro: 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.
In Vivo: 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.
相关产品:Covalent Screening Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | NF-κB Signaling Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | CNS-Penetrant Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Covalent Screening Library | Antioxidant Compound Library | Differentiation Inducing Compound Library | Oxygen Sensing Compound Library | Ubiquitination Compound Library | Pyroptosis Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Obesity Compound Library | Transcription Factor-Targeted Library | Anti-Liver Cancer Compound Library | Antidepressant Compound Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Pain-Related Compound Library | Cysteine Targeted Covalent Library | Cysteine Targeted Covalent Fragment Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | SY-5609 | BRD4 Inhibitor-18 | SJB3-019A | 8α-Tigloyloxyhirsutinolide 13-O-acetate | USP8-IN-2 | SJB2-043 | AAPK-25 | Dutasteride-13C6 | Oleic acid-13C | Anticancer agent 120 | Abacavir sulfate | Meloxicam-d3-1 | Thailanstatin D | SB-218078 | Toyocamycin | USP7-IN-1 | Sorafenib-d4 | IMD-ferulic | Busulfan | Karacoline | PTC-028 | USP7-IN-8 | 5-Hydroxy tryptophol β-D-glucuronide-d4 | Dinaciclib | CR-1-31-B | 142I5 | Farudodstat | Ecteinascidin 770 | AT9283 | Staurosporine
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货号: HY-13453
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