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.
Images & Validation
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Key Properties
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CAS Number
19542-67-7
MW
207.249
Purity
>98% (HPLC)
Formula
C10H9NO2S
SMILES
N#C/C=C/S(=O)(C1=CC=C(C)C=C1)=O
Target
NF-κB
Solubility
10 mM in DMSO
Bioactivity
−
In Vivo
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.
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