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BAY 11-7082 (BAY 11-7821) Inhibiteur de NF-κB

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

Réf. CatalogueS2913

BAY 11-7082 (BAY 11-7821) est un inhibiteur de NF-κB, qui inhibe la phosphorylation d'IκBα induite par le TNFα avec une IC50 de 10 μM dans les cellules tumorales. BAY 11-7082 inhibe la protéase spécifique de l'ubiquitine USP7 et USP21 avec une IC50 de 0,19 μM et 0,96 μM, respectivement. BAY 11-7082 induit l'apoptose et l'arrêt en phase S dans les cellules de cancer gastrique.

BAY 11-7082 (BAY 11-7821) NF-κB inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 207.25

Aller à

Contrôle Qualité

Lot : Pureté : 99.98%

99.98

Cibles apparentées	HDAC Antioxidant ROS IκB/IKK Nrf2 AP-1 MALT NOD
Autre NF-κB Inhibiteurs	DCZ0415 Omaveloxolone (RTA-408) JSH-23 QNZ (EVP4593) Caffeic Acid Phenethyl Ester SC75741 DHA (Dihydroartemisinin) Withaferin A (WFA) Andrographolide Evodiamine

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Formulation	Description de lactivité	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
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Informations chimiques, stockage et stabilité

Poids moléculaire	207.25	Formule	C₁₀H₉NO₂S	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	19542-67-7	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	BAY 11-7821			Smiles	CC1=CC=C(C=C1)S(=O)(=O)C=CC#N

Solubilité

In vitro
Lot:

DMSO : 41 mg/mL (197.82 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 10 mg/mL

Water : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

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 abroge complètement et spécifiquement la liaison de l'ADN de NF-κB, régulant à la baisse la cytokine NF-κB-inductible IL-6 et induisant l'apoptose. Ce composé (< 8 μM) est capable d'inhiber efficacement l'activité luciférase de NFκB basale et stimulée par le TNFα de manière dose-dépendante. Il (8 μM) inhibe fortement le taux de prolifération des cellules NCI-H1703. Ce composé (5 μM) réduit rapidement et efficacement la liaison de l'ADN de NF-kappaB dans les lignées de cellules T infectées par le HTLV-I et régule à la baisse l'expression du gène anti-apoptotique, Bcl-x(L), alors qu'il a peu d'effet sur la liaison de l'ADN d'un autre facteur de transcription, AP-1. Cette apoptose des cellules ATL primaires induite chimiquement est plus prononcée que celle des cellules mononucléaires du sang périphérique normales, et l'apoptose de ces cellules est également associée à une régulation à la baisse de l'activité NF-kappaB. Il (5 μM) induit sélectivement l'apoptose des lignées de cellules T infectées par le HTLV-I associée à une régulation à la baisse de l'expression de la cycline D1, de la cycline D2 et de Bcl-xL. Ce composé (100 μM) empêche la translocation nucléaire de p65 déclenchée par le NMDA et l'augmentation de la liaison de NF-κB induite par le NMDA dans les tranches hippocampiques de souris. Il prévient la toxicité du NMDA survenant dans la région CA1 des tranches hippocampiques avec une neuroprotection de 40 % à 20 μM et une neuroprotection de 70 % à 100 μM. Cette substance chimique, à toutes les concentrations testées, inhibe significativement l'activité de liaison de l'ADN de NF-κB p65 dans le tissu adipeux, tandis que dans le muscle squelettique, à 50 μM et 100 μM, elle inhibe significativement l'activité de liaison de l'ADN de NF-κB p65. Elle (100 μM) réduit la protéine IKK-β dans le tissu adipeux humain et le muscle squelettique. Ce composé (100 μM) diminue significativement la libération de TNF-α par le tissu adipeux, tandis que la libération d'IL-6 et d'IL-8 est significativement inhibée à toutes les concentrations de cette substance chimique testées. Il (50 μM) diminue significativement la libération de TNF-α, d'IL-6 et d'IL-8 dans le muscle squelettique. Ce composé est également réputé inactiver les enzymes de conjugaison E2 Ubc (ubiquitin conjugating) 13 et UbcH7 et la ligase E3 LUBAC (linear ubiquitin assembly complex), et induit ainsi la mort des lymphomes à cellules B et des leucémies à cellules T.
In vivo	BAY 11-7082, un inhibiteur de NF-κB, induit l'apoptose et l'arrêt en phase S dans les cellules de cancer gastrique.
Références	[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

Méthodes	Biomarqueurs	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

Support technique

Instructions de manipulation

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