Fig. 1 · Structure

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BAY 11-7085

Cat. No. A12470 CAS 196309-76-9

IκB/IKK inhibitor

BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM

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Publications for BAY 11-7085

1 publication citing this product

  1. Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055

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Biological Activity

Target & Activity

Target Activity Value
IκBα?phosphorylation 10 μM

Cellular Effect

Cell Line Activity Value Description Reference
A2780 EC50 2.6 μM Cytotoxicity against human A2780 cells co-cultured with human mesothelial cells after 4 hrs by firefly luciferase assay relative to control [PMID: 25581261]
A2780 IC50 2.6 μM Antitumor activity against human A2780 cells co-cultured with mesothelial cell monolayers by firefly luciferase reporter gene assay [PMID: 22326395]
BXPC-3 EC50 3.5 μM Cytotoxicity against human BxPC3 cells co-cultured with human mesothelial cells after 4 hrs by firefly luciferase assay relative to control [PMID: 25581261]
BXPC-3 IC50 3.7 μM Antitumor activity against human BxPC3 cells co-cultured with mesothelial cell monolayers by firefly luciferase reporter gene assay [PMID: 22326395]
DBTRG-05MG IC50 5.53 μM Cytotoxicity against human DBTRG-05MG cells assessed as inhibition of cell viability incubated for 24 hrs by sulforhodamine B assay [PMID: 36332549]
MDA-MB-231 IC50 4.31 μM Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 24 hrs by sulforhodamine B assay [PMID: 36332549]
SK-OV-3 EC50 5 μM Cytotoxicity against human SKOV3 cells co-cultured with human mesothelial cells after 4 hrs by firefly luciferase assay relative to control [PMID: 25581261]
SK-OV-3 IC50 7.6 μM Antitumor activity against human SKOV3 cells co-cultured with mesothelial cell monolayers by firefly luciferase reporter gene assay [PMID: 22326395]

In Vitro Studies

In HUVECs, BAY 11-7085 blocked spike- and TNFα-induced p65 nuclear translocation. In HeLa cells exposed to hTNFα and LPEI polyplexes, BAY 11-7085 treatment reduced nuclear p3NF-luc-3NF copies, while nuclear pTAL-luc copies did not statistically change; similar observations were reported with HIS-polyplexes. In Tb cells, BAY 11-7085 inhibited migration by 24.8% after 24 hours. [1,2,3]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Stimulus-induced nuclear translocation in HUVECs

Cell-based study · HUVECs [1]

HUVECs received 5 μM BAY 11-7085 before incubation with spike or TNFα. BAY 11-7085 blocked p65 nuclear translocation induced by either stimulus.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
immunofluorescence detection of NF-κB (p65)Reported result BAY 11-7085 (5 μM): blocked the nuclear translocation of p65 induced by both spike and TNFα.[1]

Literature-Reported Treatment Conditions

Treatment concentration
5 μM
Exposure duration
added 30 min before a 30 min incubation with spike (100 nM) or TNFα (1 nM)
Method
added
Co-treatment
Other interventions in this design: spike 100 nM; fibronectin 1 μg cm−1. Compound effect isolated by the comparison: spike (100 nM) or TNF⍺ (1 nM) alone or in combination with anti-α5 antibodies or the NF-κB inhibitor, BAY 11-7085.
Reported limits
Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: BAY 11-7085

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Spike-induced leukocyte adhesion to ECs is dependent on integrin α5β1–mediated NF-κB activation (S32, S34); Experimental procedures > NF-κB nuclear translocation analysis (S130, S132)

immunofluorescence detection of NF-κB (p65): immunofluorescence detection of NF-κB (p65); comparator: spike (100 nM) or TNF⍺ (1 nM) alone — Results > Spike-induced leukocyte adhesion to ECs is dependent on integrin α5β1–mediated NF-κB activation (S32, S34); Experimental procedures > NF-κB nuclear translocation analysis (S132)

Nuclear plasmid copies in HeLa cells

Cell-based study · HeLa cells [2]

HeLa cells were pre-treated with 1 µM BAY 11-7085 for 1 h at 37°C. LPEI (A): the number of p3NF-luc-3NF copies in the nucleus at 1, 3 and 5 h clearly decreased and was 4-fold lower than in untreated cells. The same procedure carried out in cells transfected with HIS-polyplexes led to similar observations.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
the number of p3NF-luc-3NF copies in the nucleusnuclear plasmid copies 1 µM BAY 11-7085; LPEI (A); 1, 3 and 5 h: 4-fold lower than in untreated cells[2]

Literature-Reported Treatment Conditions

Treatment concentration
1 µM
Exposure duration
HeLa cells were pre-treated with 1 µM BAY 11-7085 for 1 h at 37°C in medium supplemented with 10% FBS, prior to incubation with 25 ng/ml hTNFα and 1 µM BAY 11-7085 at 37°C in the presence of fluo-pTAL-luc/LPEI and Cy3-p3NF-luc-3NF/LPEI polyplexes. The cells were then observed under confocal microscopy in real-time after 1 h, 3 h and 5 h incubation.
Method
pre-treated
Co-treatment
Other interventions in this design: hTNFα 25 ng/ml; Draq5 1 µM. Compound effect isolated by the comparison: in the absence or the presence of BAY 11-7085.
Reported limits
Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: BAY 11-7085

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

MATERIALS AND METHODS > CLSM (S47); MATERIALS AND METHODS > Plasmid quantitation in cell nucleus (S52, S57, S58); RESULTS > Nuclear quantitation of pDNA > NFκB inhibition (S181, S182, S183); Figure 8. legend (S236, S237, S239)

the number of p3NF-luc-3NF copies in the nucleus: the number of p3NF-luc-3NF copies in the nucleus; comparator: Cells were also transfected in the absence of BAY 11-7085 with Cy3-p3NF-luc-3NF polyplexes (solid bar) and fluo-pTAL-luc polyplexes (open bar). — MATERIALS AND METHODS > Plasmid quantitation in cell nucleus (S57); RESULTS > Nuclear quantitation of pDNA > NFκB inhibition (S181, S182, S183); Figure 8. legend (S236)

Migration inhibition in Tb cells

Cell-based study · Tb [3]

Tb cells were treated with 10 μM BAY 11-7085 in the upper chamber for 24 hours. Cell migration was inhibited by 24.8% relative to vehicle-treated cells.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
cell migrationcell migration Tb; 10 μM BAY 11-7085; 24 hours: 24.8%[3]

Literature-Reported Treatment Conditions

Treatment concentration
10 μM
Exposure duration
24 hours
Method
placed in the upper chamber
Reported limits
Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: BAY 11-7085

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Methods > Cell migration assays (S61, S62, S63); Results > Suppression of Cell Migration in SCCHN Cells Treated with PDTC or BAY 11-7085 (S118, S119)

cell migration: cell migration; comparator: Treated cells with the vehicles of above reagents — Methods > Cell migration assays (S61, S63); Results > Suppression of Cell Migration in SCCHN Cells Treated with PDTC or BAY 11-7085 (S118, S119)

In Vivo Studies

Female Balb/Cnu/nu mice injected with TL cells into the foot pads received BAY 11-7085 intraperitoneally at 5 mM/kg/day for 14 days. The BAY 11-7085 group had fewer lymph nodes with metastases than the PBS control group. [3]

Lymph node metastases in mice receiving TL cells

Animal study · Female 4- to 5-week-old Balb/Cnu/nu mice; TL cells were harvested and injected into the foot pads [3]

Female Balb/Cnu/nu mice injected with TL cells into the foot pads received BAY 11-7085 intraperitoneally at 5 mM/kg/day for 14 days. The BAY 11-7085 group had fewer lymph nodes with metastases than the PBS control group.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
The number of lymph nodes with metastaseslymph nodes with metastases 5 mM/kg/day of BAY 11-7085 for 14 days: one lymph node[3]

Conditions shared by the study groups

Route
intraperitoneally (i.p)
Treatment course
Three weeks after injection; for 14 days
Vehicle
100 μl PBS
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
BAY 11-7085 5 mM/kg/dayControl animals received 100 μl PBS alone.In the control group, eight lymph nodes were positive for lymph node metastases, whereas two of the lymph nodes in the PDTC group had metastases, and one lymph node in the BAY 11-7085 group contained a metastasis[3]
BAY 11-7085 5 mM/kg/day
Model: Female 4- to 5-week-old Balb/Cnu/nu mice; TL cells were harvested and injected into the foot pads
Methods and source locations

Compound reported in the paper: BAY 11-7085

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Methods > Mice Injected with TL Cells and PDTC or BAY 11-7085 Treatment (S80, S82, S83, S84, S89); Results > Decreased Hematologic and lymphatic Metastasis of SCCHN Cell Lines Following Inhibition of NF-κB (S128, S130)

The number of lymph nodes with metastases: The number of lymph nodes with metastases; comparator: Control animals received 100 μl PBS alone. — Methods > Mice Injected with TL Cells and PDTC or BAY 11-7085 Treatment (S83, S89); Results > Decreased Hematologic and lymphatic Metastasis of SCCHN Cell Lines Following Inhibition of NF-κB (S130)

BAY 11-7085 5 mM/kg/day · Methods > Mice Injected with TL Cells and PDTC or BAY 11-7085 Treatment (S83); Results > Decreased Hematologic and lymphatic Metastasis of SCCHN Cell Lines Following Inhibition of NF-κB (S130)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 196309-76-9
Applications IκB/IKK inhibitor
Formula C13H15NO2S
Molecular Weight 249.33
Synonyms Bay 11-7083
SMILES
CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)/C=C/C#N

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 49 mg/mL (196.52 mM)
Water Insoluble
Ethanol 49 mg/mL (196.52 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Robles JP, Zamora M, Adan-Castro E, et al. The spike protein of SARS-CoV-2 induces endothelial inflammation through integrin α5β1 and NF-κB signaling. J Biol Chem (2022). PMID: 35143839 DOI: 10.1016/j.jbc.2022.101695 Source material
  2. [2] Breuzard G, Tertil M, Gonçalves C, et al. Nuclear delivery of NFkappaB-assisted DNA/polymer complexes: plasmid DNA quantitation by confocal laser scanning microscopy and evidence of nuclear polyplexes by FRET imaging. Nucleic Acids Res (2008). PMID: 18515353 DOI: 10.1093/nar/gkn287 Source material
  3. [3] Yan M, Xu Q, Zhang P, et al. Correlation of NF-kappaB signal pathway with tumor metastasis of human head and neck squamous cell carcinoma. BMC Cancer (2010). PMID: 20716363 DOI: 10.1186/1471-2407-10-437 Source material

Publications

1 publication citing this product

  1. Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055

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