BAY 11-7082

Description

Biological Activity

Protocol(Only for Reference)

Chemical Information

Cell Assay: [2]

References

貨號 Cat. No.: S2913
規格 Size: 10mM/1mL~500mg
品牌 Brand: Selleckchem

BAY 11-7082

Catalog No.S29131 Product Citations

BAY 11-7082 is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM.

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 151	In stock	0 1 2 3 4 5 6 7 8 9 10
10mg	USD 113	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 340	In stock	0 1 2 3 4 5 6 7 8 9 10

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Cell lines	NCI-H1703 cells
Concentrations	~8 μM
Incubation Time	12 hours
Method	Cells are transfected with siRNA in 96-well microtiter plates and then cultured for 72 hours in complete NSCLC medium, treated with BAY 11-7082 for 12 hours. Cells are incubated with [3H]thymidine for 3 hours. The cells are collected on filters using an automatic cell harvester and radioactivity on the filters is measured by β-scintillation counting.

Description

BAY 11-7082 is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM.

In vitro

BAY 11-7082 completely and specifically abrogates NF-κB DNA binding, downregulating the NF-κB-inducible cytokine IL-6 and inducing apoptosis. [1] BAY 11-7082 (< 8 μM) is able to effectively inhibit both basal and TNFα stimulated NFκB luciferase activity in a dose dependent manner. BAY 11-7082 (8 μM) strongly inhibits the rate of proliferation in NCI-H1703 cells. [2] Bay 11-7082 (5 μM) rapidly and efficiently reduces the DNA binding of NF-kappaB in HTLV-I-infected T-cell lines and down-regulates the expression of the antiapoptotic gene, Bcl-x(L), whereas it has little effect on the DNA binding of another transcription factor, AP-1. Bay 11-7082-induced apoptosis of primary ATL cells is more prominent than that of normal peripheral blood mononuclear cells, and apoptosis of these cells is also associated with down-regulation of NF-kappaB activity. Bay 11-7082 (5 μM) selectively induces apoptosis of HTLV-I–infected T-cell lines associated with down-regulation of the expression of cyclin D1, cyclin D2, and Bcl-xL. [3] BAY 11-7082 (100 μM) prevents the nuclear translocation of p65 elicited by NMDA and the NMDA-induced increase of NF-κB binding in mouse hippocampal slices. BAY 11-7082 prevents NMDA toxicity occurring in CA1 region of hippocampal slices with 40% neuroprotection at 20 μM and 70% neuroprotection at 100 μM. [4] BAY 11-7082 at all concentrations tested significantly inhibits NF-κB p65 DNA-binding activity in adipose tissue, whereas in skeletal muscle, BAY 11-7082 at 50 μM and 100 μM significantly inhibits NF-κB p65 DNA-binding activity. BAY 11-7082 (100 μM) reduces IKK-β protein in human adipose tissue and skeletal muscle. BAY 11-7082 (100 μM) significantly decreases the release of TNF-α from adipose tissue, whereas the release of IL-6 and IL-8 is significantly inhibited at all concentrations of BAY 11-7082 tested. BAY 11-7082 (50 μM) significantly decreases the release of TNF-α, IL-6, and IL-8 in skeletal muscle. [5] BAY 11-7082 (3.5 mM) inhibits constitutive NF-kappaB activity in the LBR-, LBR-D160 and LBR-V160 cells. BAY 11-7082 induces a higher percentage of apoptosis in LBR-V160 and LBR-D160 cells than in LBR- cells. BAY 11-7082 (3.5 mM) is able to induce a slight decrease in IL-10 mRNA in the LBR-, LBR-D160 and LBR-V160 cells whereas a slight increase in IL-15, TGF-β1 and TNF-α expression is observed. [6]

Download BAY 11-7082 SDF Download BAY 11-7082 SDF

Molecular Weight (MW)	207.25
Formula	C10H9NO2S
CAS No.	19542-67-7

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	41 mg/mL (197 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	10 mg/mL (48 mM)
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol,	15 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.