BAY 11-7082

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BAY 11-7082 一种 NF-κB 抑制剂，可选择性且不可逆地抑制 TNF-α 诱导的 IκBα 磷酸化 (IC50=10 uM)。

BAY 11-7082 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; 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; selectively inhibits Tax-induced NF-κB activity in a human T-cell line.(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):TAK-659 hydrochloride (100 mg/kg/day; p.o.; daily, for 10 days) treatment totally abrogates splenomegaly and tumor development in LMP2A/MYC mice in both pretumor and tumor cell transfer experiments.TAK-659 hydrochloride treatment kills tumor cells, but not host cells within the spleen and tumors.TAK-659 hydrochloride treatment abrogates metastasis of tumor cells into bone marrow.

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Animal Model:Four-week-old male BALB/c nude mice with human gastric carcinoma cell lines HGC-27 Dosage:Low-dose (2.5 mg/kg body weight), high-dose (5 mg/kg body weight) Administration:Intratumoral injection; twice-weekly for 21 days Result:Suppressed tumor growth in a dose-dependent manner.

BAY 11-7821

Apoptosis

NF-κB

E2-conjugatingenzymes|IκBα?phosphorylation

Inflammation/Immunology

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19542-67-7

207.249

C10H9NO2S

>98% (HPLC)

10 mM in DMSO

N#C/C=C/S(=O)(C1=CC=C(C)C=C1)=O

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

(-20℃)

With Ice Pack

≥ 2 years