research use only

BAY 11-7082 (BAY 11-7821) NF-κB Inhibitor

Name: BAY 11-7082 (BAY 11-7821)
Brand: Selleck Chemicals
SKU: S2913
Availability: InStock
Rating: 5 (394 reviews)

Cat.No.S2913

BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.

Chemical Structure

Molecular Weight: 207.25

Jump to

Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	HDAC Antioxidant ROS IκB/IKK Nrf2 AP-1 MALT NOD
Other NF-κB Inhibitors	DCZ0415 Omaveloxolone (RTA-408) JSH-23 QNZ (EVP4593) Caffeic Acid Phenethyl Ester SC75741 DHA (Dihydroartemisinin) Withaferin A (WFA) Andrographolide CBL0137

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
HeLa	Function Assay	10 μM	1.5 h		abolishes BPA induced up regulation of FN and MMP-9	25797437
SiHa	Function Assay	10 μM	1.5 h		abolishes BPA induced up regulation of FN and MMP-9	25797437
ARPE-19	Function Assay	1 μM	0.5 h		suppresses TG-induced IL-8 promoter activation	25593029
HCT116	Function Assay	5 μM	2 h	DMSO	attenuates silymarin-induced downregulation of cyclin D1	25479723
HMECs	Function Assay	5 μM	2 h		abolishes TNF-α-induced VCAM-1 expression	25193116
A549	Function Assay	10 µM	12 h		suppresses Dvl-3 induced activation of p65	25156800
RAW 264.7	Function Assay	5 μM	1 h		inhibits TNF-α and IL-12 p40 production	25019567
macrophages	Function Assay	5 µM	3 h		partially blocks YPFS-induced expression of iNOS and COX-2	24967898
HUVECs	Function Assay	3-30 μM	1 h		reduces the expression of miR-146a in a dose-dependent manner	24863965
HeLa	Function Assay	5 μM	24 h	DMSO	reduces the activity of TNF-α promoter	24657783
A549	Function Assay	10 μM	1 h		inhibits the increase of phospho-IκBα in PA103-infected cultures	24612488
HUVEC	Function Assay	20 µM	0.5 h	DMSO	prevents the induction of EAM expression	24551209
A549RT-eto	Apoptosis Assay	10 μM	24 h	DMSO	accelerates FERO-mediated apoptosis	24535083
THP-1	Function Assay	0.1/1 μM	0.5 h		abrogates TNF-α secretion as well as the increased secretion of IL-6 and IL-1β	24378536
SKCXCR2	Growth Inhibition Assay	2 µM	48 h		decreases cell proliferation significantly	24376747
SKCXCR2	Function Assay	2 µM	48 h		blocks the CXCL1-induced cell invasion	24376747
OVCXCR2	Function Assay	2 µM	48 h		blocks the CXCL1-induced cell invasion	24376747
DSCs	Function Assay	2.5 μM	0.5 h		reverses the enhancement of CCL2/CCR2 expression of DSCs induced by IL-33	24344240
WPs	Function Assay	25 μM	5 min		suppresses ATP and vWF secretion	24331207
A549RT-eto	Apoptosis Assay	10 μM	24 h		accelerates F14 extract-mediated apoptosis combined treatment with F14	24220725
A549RT-eto	Function Assay	10 μM	24 h		decreases the expression levels of NF-κB and P-gp	24220725
FaDu	Function Assay		2 h		inhibits p65 expression and blocks TNFα-induced TWIST expression	24220622
IVD	Function Assay	10 μM	3 d		reverses TNF-α–mediated suppression of the disc matrix macromolecules aggrecan and collagen II	24176808
IVD	Function Assay	10 μM	3 d		abrogates TNF-α–induced up-regulation of ADAMTS-4 and ADAMTS-5	24176808
iNKT	Function Assay	10/100 μM	0.5 h		inhibits the induction of A2AR mRNA and other factor	24124453
PC-3	Function Assay	2.5/5/10 μM	0.5 h		blocks IGF-II-induced STS mRNA expression	24055520
THP-1	Function Assay	10 μM	1 h		abolishes the effect of rHSP27 on SR-A mRNA	23939398
A549	Function Assay	1 μM	48 h		enhances the up-regulation of IκB and subsequent decrease in Bax expression induced by combined stimulation	23900080
A549	Apoptosis Assay	1 μM	48 h		reduces the cell death induced by combined stimulation	23900080
NCI-N87	Growth Inhibition Assay	10/20/30 μM	6/24 h		suppresses cell viability significantly	23846545
AGS	Growth Inhibition Assay	10/20/30 μM	6/24 h		suppresses cell viability significantly	23846545
MGC80-3	Growth Inhibition Assay	10/20/30 μM	6/24 h		suppresses cell viability significantly	23846545
HGC-27	Function Assay	7.5/15/30 μM	6 h		induces the dephosphorylation and up-regulation of IκBα	23846545
MGC80-3	Function Assay	7.5/15/30 μM	6 h		induces the dephosphorylation and up-regulation of IκBα	23846545
HGC-27	Apoptosis Assay	7.5/15/30 μM	6 h		induces apoptosis in a time- and dose-dependent manner	23846545
HBE	Function Assay	10μM	3h		abolishes the increases of IL-6 expression induced by CSE	23824089
HepG2	Function Assay	0.3/1/3 μM	48 h		reduces IL6-induced PON1 expression	23791833
THP-1	Function Assay	5 µM	1 h	DMSO	inhibits MTB-induced NFκB activation	23634218
THP-1	Growth Inhibition Assay	5 µM	4/8 d	DMSO	reduces the viability of intracellular MTB	23634218
MDM	Growth Inhibition Assay	5 µM	4/8 d	DMSO	reduces the viability of intracellular MTB	23634218
AM	Growth Inhibition Assay	5 µM	4/8 d	DMSO	reduces the viability of intracellular MTB	23634218
RAW 264	Function Assay	0.2-5 µM	30/60/90 min		inhibits the phosphatase activity of PTP1B	23578302
HUVEC	Function Assay	10 μM	0.5 h	DMSO	counteractes the loss of Tie2 mRNA	23563632
HT29	Function Assay	10/30/100 μM	1 h		inhibites both TWEAK-induced p100 processing	23527154
HT29	Function Assay	10/30/100 μM	1 h		inhibits TNF-induced phosphorylation and degradation of IκBα	23527154
MM.1S	Apoptosis Assay	30 µM	3 h		induces MM cell death involves necrosis	23527154
KMS-12-BM	Apoptosis Assay	30 µM	3 h		induces MM cell death involves necrosis	23527154
BAFs	Function Assay	0.5/1 μM	24 h		inhibits TNFα/DEX induced CYP19A1 transcripts	23485457
SP6.5	Function Assay	5 μM	2 h		decreases translocation of p65 in the nucleus	23443086
VUP	Function Assay	5 μM	2 h		decreases translocation of p65 in the nucleus	23443086
OCM1	Function Assay	5 μM	2 h		decreases translocation of p65 in the nucleus	23443086
OM431	Function Assay	5 μM	2 h		decreases translocation of p65 in the nucleus	23443086
SP6.5	Growth Inhibition Assay	2.5-20 μM	24 h		IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
VUP	Growth Inhibition Assay	2.5-20 μM	24 h		IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
OCM1	Growth Inhibition Assay	2.5-20 μM	24 h		IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
OM431	Growth Inhibition Assay	2.5-20 μM	24 h		IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
SP6.5	Apoptosis Assay	5 μM	24 h		induces apoptosis	23443086
VUP	Apoptosis Assay	5 μM	24 h		induces apoptosis	23443086
OCM1	Apoptosis Assay	5 μM	24 h		induces apoptosis	23443086
OM431	Apoptosis Assay	5 μM	24 h		induces apoptosis	23443086
SP6.5	Function Assay	5 μM	12 h		reduces the migration	23443086
VUP	Function Assay	5 μM	12 h		reduces the migration	23443086
OCM1	Function Assay	5 μM	12 h		reduces the migration	23443086
OM431	Function Assay	5 μM	12 h		reduces the migration	23443086
HBL-1	Growth Inhibition Assay	3 μM	24/48/72 h	DMSO	slows cell growth modestly	23441730
RAW 264.7	Function Assay	2-15 μM	1 h	DMSO	suppresses the activation of IKK family members	23441730
IL-1R	Function Assay	2-15 μM	1 h	DMSO	suppresses the activation of IKK family members	23441730
RAW 264.7	Function Assay	15 μM	1 h	DMSO	suppresses the activation of and JNK	23441730
IL-1R	Function Assay	15 μM	1 h	DMSO	suppresses the activation of and JNK	23441730
U2OS	Function Assay	15 μM	1 h	DMSO	prevents the LPS- or IL-1-stimulated formation of K63-pUb chains	23441730
MT‐1	Function Assay	8 µm	3 h		decreases the levels of p‐STAT3 and p‐4EBP1	23278479
MT‐2	Function Assay	8 µm	3 h		decreases the levels of p‐STAT3 and p‐4EBP1	23278479
MT‐1	Function Assay	8 µm	3 h		decreases the levels of the p65 subunit of NF‐κB	23278479
MT‐2	Function Assay	8 µm	3 h		decreases the levels of the p65 subunit of NF‐κB	23278479
MCF-7	Function Assay	2.5-15 μM	0.5 h	DMSO	causes the gradual loss of cell adhesion	23093227
HaCaT	Function Assay	5.0 μM	1 h		attenuates the TCOH-induced production of IL-6	23041168
A549	Function Assay		1 h		inhibits LTA-induced SP-A mRNA production significantly	23031213
OA chondrocytes	Function Assay	10 μM	1 h		blocks the AGE-BSA-induced gene/protein expression of GRP78 or COX-2 (p<0.05)	22982228
RAW264.7	Function Assay	15 μM	15-120 min		blocks the production of NO, PGE2, and TNF-α	22745523
RAW264.7	Growth Inhibition Assay	5-30 μM	24 h		inhibits cell growth in a dose-dependent manner	22745523
HBL6	Apoptosis Assay	0.5/5/25 μM	6/24 h		decreases cell viability and leeads to apoptosis in a dose-dependent manner	22074820
HT29	Function Assay	1-10 μM	10 h		increases HO-1 mRNA and protein expression	21620964
Ca9–22	Apoptosis Assay	10 μM	1 h		completely inhibits ALA-PDT-induced apoptosis	21138480
Ca9–22	Function Assay	10 μM	1 h		completely abrogates the ALA-PDT-induced JNK activation	21138480
A-549	Growth Inhibition Assay	10 μM	24/48 h		inhibits cell growth in a time-dependent manner	20866043
AP	Function Assay	5/10 μM	48 h		downregulates the BAD protein level a dose-dependent manner	20596645
AQ1	Function Assay	5/10 μM	48 h		downregulates the BAD protein level a dose-dependent manner	20596645
AP	Function Assay	20 μM	4/8 h		downregulates the BAD protein level a time-dependent manner	20596645
AQ1	Function Assay	20 μM	4/8 h		downregulates the BAD protein level a time-dependent manner	20596645
THP-1	Function Assay	5 μM	0.5 h		attenuates the LPS-induced p-IκBα protein by 72%	20309718
K562	Growth Inhibition Assay	2-30 μM	24 h		IC50=8 μM,inhibits cell growth in a dose-dependent manner	19646807
Jurket	Growth Inhibition Assay	2-30 μM	24 h		IC50=7.1 μM, inhibits cell growth in a dose-dependent manner	19646807
U937	Growth Inhibition Assay	2-30 μM	24 h		IC50=10.5 μM, inhibits cell growth in a dose-dependent manner	19646807
PBMC	Growth Inhibition Assay	2-30 μM	24 h		IC50=40.2 μM, inhibits cell growth in a dose-dependent manner	19646807
K562	Apoptosis Assay	2-20 μM	24 h		induces a dose-dependent apoptosis	19646807
THP1	Cytotoxicity assay		72 hrs		Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 72 hrs by MTT assay, TC50 = 1.5 μM.	28410442
RAW264.7	Function assay		6 hrs		Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells treated 30 mins before LPS challenge measured after 6 hrs by luciferase reporter gene assay, IC50 = 1.72 μM.	24315191
HEK293	Function assay		6 hrs		Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM.	24533857
HEK293	Function assay		6 hrs		Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM.	24992702
HEK293	Function assay		6 hrs		Inhibition of TNFalpha-induced NF-kappaB activity (unknown origin) transfected in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM.	26343828
HEK293	Function assay		6 hrs		Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM.	22850207
HEK293	Function assay		6 hrs		Inhibition of TNFalpha-induced human NFkappaB activity in HEK293 cells incubated for 6 hrs followed by compound wash out measured after 5 mins by by luciferase assay, IC50 = 2.01 μM.	22712432
HEK293	Cytotoxicity assay				Cytotoxicity against HEK293 cells, IC50 = 3.8 μM.	24533857
HEK293	Function assay		6 hrs		Inhibition of TNFalpha-induced NFkappaB (unknown origin) activation expressed in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 5 μM.	23316950
HEK293	Function assay				Effect on Cdc2 expressed in HEK293 cells assessed as effect on Cdc2:Cdc25C interaction complexes in presence of camptothecin by EYFP and/or YFP Venus fragment based reporter gene assay	16680159
HEK293	Function assay	20 uM	24 hrs		Inhibition of TNF-alpha stimulated NFkappaB transactivation in HEK293 cells at 20 uM measured after 24 hrs by dual luciferase reporter gene assay	27736063
RAW264.7	Function assay	20 uM	1 hr		Inhibition of LPS-induced NFkB activation in mouse RAW264.7 cells assessed as reduction in nuclear translocation of p65 at 20 uM preincubated for 1 hr followed by LPS stimulation measured after 3 hrs by Western blot method	28667873
RAW264.7	Function assay	20 uM	6 hrs		Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells at 20 uM treated 30 mins before LPS challenge measured after 6 hrs by luciferase reporter gene assay	24315191
RAW264.7	Antinflammatory assay	20 uM	18 hrs		Antinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 20 uM treated 30 mins before LPS challenge measured after 18 hrs by Griess assay	24315191
THP1	Antinflammatory assay	5 uM	24 hrs		Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced extracellular IL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA	24400858
THP1	Antinflammatory assay	5 uM	24 hrs		Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced extracellular TNF-alpha production at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA	24400858
THP1	Antinflammatory assay	5 uM	24 hrs		Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced intracellular proIL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA	24400858
THP1	Antinflammatory assay	5 uM	24 hrs		Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced intracellular IL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA	24400858
RAW264.7	Function assay	0.3 ug/ml	12 hrs		Inhibition of LPS-induced NF-kB p65 phosphorylation in mouse RAW264.7 cells at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method	28284806
RAW264.7	Function assay	0.3 ug/ml	12 hrs		Inhibition of LPS-induced NF-kB p65 activation in mouse RAW264.7 cells at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by DAPI staining based inverted fluorescence microscopic method	28284806
RAW264.7	Function assay	0.3 ug/ml	12 hrs		Inhibition of NF-kB p65 in mouse RAW264.7 cells assessed as reduction in LPS-induced iNOS expression at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method	28284806
RAW264.7	Function assay	0.3 ug/ml	12 hrs		Inhibition of NF-kB p65 in mouse RAW264.7 cells assessed as reduction in LPS-induced COX2 expression at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method	28284806
HEK293	Function assay	20 uM	24 hrs		Inhibition of TNFalpha-induced NFkappaB activation in HEK293 cells at 20 uM after 24 hrs by dual luciferase reporter gene assay	28873303
RAW264.7	Function assay	20 uM	2 hrs		Inhibition of NFkappaB nuclear translocation in LPS-stimulated mouse RAW264.7 cells at 20 uM pretreated for 2 hrs followed by LPS-induction by DAPI-staining based immunofluorescence microscopic method	29759725
BGC823	Function assay	5 uM	12 hrs		Inhibition of colony formation in human BGC823 cells at 5 uM treated for 12 hrs followed by incubation in drug free medium for 14 days by crystal violet staining based assay	28881286
SGC7901	Function assay	5 uM	12 hrs		Inhibition of colony formation in human SGC7901 cells at 5 uM treated for 12 hrs followed by incubation in drug free medium for 14 days by crystal violet staining based assay	28881286
RAW264.7	Function assay	10 uM	2 hrs		Inhibition of LPS-induced IL-6 mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method	27038497
RAW264.7	Function assay	10 uM	2 hrs		Inhibition of LPS-induced IL-1beta mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method	27038497
RAW264.7	Function assay	10 uM	2 hrs		Inhibition of LPS-induced iNOS mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method	27038497
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 41 mg/mL (197.82 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (19.30mM)	Taking the 1 mL working solution as an example, add 100 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	8.000mg/ml (38.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 160 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (9.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	207.25	Formula	C₁₀H₉NO₂S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	19542-67-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BAY 11-7821			Smiles	CC1=CC=C(C=C1)S(=O)(=O)C=CC#N

Mechanism of Action

Targets/IC₅₀/Ki	E2-conjugating enzymes (Cell-free assay) USP7 (Cell-free assay) 0.19 μM USP21 (Cell-free assay) 0.96 μM USP6 (Cell-free assay) 1.7 μM IκBα phosphorylation (Tumor cells) 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. This compound (< 8 μM) is able to effectively inhibit both basal and TNFα stimulated NFκB luciferase activity in a dose dependent manner. It (8 μM) strongly inhibits the rate of proliferation in NCI-H1703 cells. This compound (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. This chemical-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. It (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. This compound (100 μM) prevents the nuclear translocation of p65 elicited by NMDA and the NMDA-induced increase of NF-κB binding in mouse hippocampal slices. It prevents NMDA toxicity occurring in CA1 region of hippocampal slices with 40% neuroprotection at 20 μM and 70% neuroprotection at 100 μM. This chemical at all concentrations tested significantly inhibits NF-κB p65 DNA-binding activity in adipose tissue, whereas in skeletal muscle, it at 50 μM and 100 μM significantly inhibits NF-κB p65 DNA-binding activity. It (100 μM) reduces IKK-β protein in human adipose tissue and skeletal muscle. This compound (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 this chemical tested. It (50 μM) significantly decreases the release of TNF-α, IL-6, and IL-8 in skeletal muscle. This compound is also found to inactivate the E2-conjugating enzymes Ubc (ubiquitin conjugating) 13 and UbcH7 and the E3 ligase LUBAC (linear ubiquitin assembly complex), and thus induces B-cell lymphoma and leukaemic T-cell death.
In vivo	BAY 11-7082, an NF-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17227230/ [2] https://pubmed.ncbi.nlm.nih.gov/22549160/ [3] https://pubmed.ncbi.nlm.nih.gov/16162000/ [4] https://pubmed.ncbi.nlm.nih.gov/12176906/ [5] https://pubmed.ncbi.nlm.nih.gov/15755516/ [6] https://pubmed.ncbi.nlm.nih.gov/23441730/ [7] https://pubmed.ncbi.nlm.nih.gov/25159004/ [8] https://pubmed.ncbi.nlm.nih.gov/23846545/

Applications

Methods	Biomarkers	Images	PMID
Western blot	NF-κB p-IKKβ/ IκBα p-IRAK4 / IRAK4 NF-κB p-IKKβ/ IκBα p-IRAK4 / IRAK4		31332209
Growth inhibition assay	Cell viability Cell viability		31332209

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):