Cat. No. Name Size Price Add Cart
KI1439Bay 11-708210 mg$144
Bay 11-708250 mg$432

Chemical Characteristic

Product NameBay 11-7082
CAS No.19542-67-7
Molecular Weight 207.25
FormulaC10H9NO2S
Chemical Name(E)-3-(4-methylphenyl)sulfonylprop-2-enenitrile
SmilesC(#N)/C=C/S(=O)(=O)c1ccc(cc1)C
Chemical Structure

Biological activities

Bay 11-7082 is an inhibitor of NF-κB. Bay 11-7082 is an irreversible inhibitor of IκBα phosphorylation with an IC50 of 10 µM.[1] The IC50 of BAY 11-7082 for HANK1, NKL and NK-92 cells is 1.8, 0.6 and 4.2 µM, respectively. [2] The IC50 of BAY 11-7082 against collagen-activated platelets is 5.6 mM. BAY 11-7082 dependently inhibits platelet aggregation with an IC50 of 5.7 mM. BAY 11-7082 inhibits ATP release and surface P-selectin expression in collagen- activated platelets. BAY 11-7082 inhibits collagen-induced TXA2 generation and intracellular Ca2+ concentration. BAY 11-7082 enhances vasodilator-stimulated-phosphoprotein (VASP) phosphorylation. BAY 11-7082 attenuates c-Jun N-terminal kinase 1 (JNK1) and extracellular-signal- regulated protein kinase 2 (ERK2) phosphorylations. [3] Bay 11-7082 induces apoptosis of HTLV-I??nfected T-cell lines and negligible apoptosis of HTLV-I??egative T cells. Bay 11-7082 rapidly and efficiently reduces the DNA binding of NF-κB in HTLV-I??nfected T-cell lines and down-regulates the expression of the antiapoptotic gene, Bcl-xL, regulated by NF-κB. [4] Bay 11-7082 has been shown to be a potent inducer of apoptosis in leukemia and lymphoma cells. Bay 11-7082 increases stabilization of IκBa and specifically blocks NF-κB signaling. Bay 11-8072 markedly potentiates UCN-01-induced apoptosis in several MM cell types, including some resistant to steroid-mediated cell death. Treatment with Bay 11-7082 (4 mM) individually for 24 hours results in significant increases in the G0/G1 cell fraction. [5] Bay 11-7082 blocks TNFa capacity to induce cell proliferation and up-regulation of cyclin D1 and of Bcl-xL in vivo. [6]

Protocols

Bay 11-7082 is dissolved in sterile DMSO and stored at -20 °C under light-protected conditions. [5]

References

[1] Melisi D, et al. NF-kappa B as a target for cancer therapy. Expert Opin Ther Targets. 2007, 11(2): 133-144.
[2] Kim K, et al. Effects of nuclear factor-kappaB inhibitors and its implication on natural killer T-cell lymphoma cells. Br J Haematol. 2005, 131(1): 59-66.
[3] Lee HS, et al. A noble function of BAY 11-7082: Inhibition of platelet aggregation mediated by an elevated cAMP-induced VASP, and decreased ERK2/JNK1 phosphorylations. Eur J Pharmacol. 2010, 627(1-3): 85-91.
[4] Mori N, et al. Bay 11-7082 inhibits transcription factor NF-kappaB and induces apoptosis of HTLV-I-infected T-cell lines and primary adult T-cell leukemia cells. Blood. 2002, 100(5): 1828-1834.
[5] Dai Y, et al. Interruption of the NF-kappaB pathway by Bay 11-7082 promotes UCN-01-mediated mitochondrial dysfunction and apoptosis in human multiple myeloma cells. Blood. 2004, 103(7): 2761-2770.
[6] Rivas MA, et al. TNF alpha acting on TNFR1 promotes breast cancer growth via p42/P44 MAPK, JNK, Akt and NF-kappa B-dependent pathways. Exp Cell Res. 2008, 314(3): 509-529.

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