BAY 11-7082 (BAY 11-7821) is an irreversible inhibitor of TNF-α-stimulated IκBα phosphorylation. BAY 11-7082 selectively and irreversibly inhibits NF-κB activation by blocking TNF-α-induced phosphorylation of IκB-α without affecting constitutive IκB-α phosphorylation. BAY 11-7082 inhibits the TNF-α-induced surface expression of adhesion molecules ICAM-1, VCAM-1, and E-selectin in human endothelial cells with IC50 values of 5-10 µM. BAY 11-7082 also reversibly activates MAP kinases and stimulates apoptosis. BAY 11-7082 rapidly and efficiently reduced the DNA binding of NF-kappaB in HTLV-I-infected T-cell lines and down-regulated the expression of the antiapoptotic gene, Bcl-x(L), regulated by NF-kappaB, whereas it had little effect on the DNA binding of another transcription factor, AP-1.
Furthermore, BAY 11-7082- induced apoptosis of primary ATL cells was more prominent than that of normal peripheral blood mononuclear cells, and apoptosis of these cells was also associated with down-regulation of NF-kappaB activity.
Foods. 2022 Jan 12;11(2):196.
Impact of the Plastein Reaction of Casein Hydrolysates in the Presence of Exogenous Amino Acids on Their Anti-Inflammatory Effect in the Lipopolysaccharide-Stimulated Macrophages
BAY 11-7082 purchased from AbMole
J Inflamm Res. 2021 Mar 17;14:917-928.
Stable Cells with NF-KB-ZsGreen Fused Genes Created by TALEN Editing and Homology Directed Repair for Screening Anti-inflammation Drugs.
BAY 11-7082 purchased from AbMole
J Inflamm Res. 2021 Mar 17;14:917-928.
Stable Cells with NF-κB-ZsGreen Fused Genes Created by TALEN Editing and Homology Directed Repair for Screening Anti-inflammation Drugs
BAY 11-7082 purchased from AbMole
Mediators Inflamm. 2019 Feb 19;2019:1082497.
Astragaloside IV Suppresses High Glucose-Induced NLRP3 Inflammasome Activation by Inhibiting TLR4/NF-κB and CaSR.
BAY 11-7082 purchased from AbMole
Molecular Weight | 207.25 |
Formula | C10H9NO2S |
CAS Number | 19542-67-7 |
Solubility (25°C) | DMSO 31 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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BAY-985
BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. |
WAY-388756
WAY-388756 is a IKKb inhibitor. |
WAY-113178
WAY-113178 is a IkB kinase-beta (IKKb) inhibitor. |
MRT67307
MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells. |
IKK-IN-1
IKK-IN-1 is an inhibitor of IKK extracted from patent WO2002024679A1, compound example 18-13. |
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