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

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

Cat.nr.S2913

BAY 11-7082 (BAY 11-7821) is een NF-κB-remmer, remt TNFα-geïnduceerde IκBα-fosforylering met een IC50 van 10 μM in tumorcellen. BAY 11-7082 remt ubiquitine-specifieke protease USP7 en USP21 met respectievelijk een IC50 van 0,19 μM en 0,96 μM. BAY 11-7082 induceert apoptose en S-fase-arrest in maagkankercellen.

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

Chemische structuur

Molecuulgewicht: 207.25

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Batch: Zuiverheid: 99.98%

99.98

Gerelateerde doelwitten	HDAC Antioxidant ROS IκB/IKK Nrf2 AP-1 MALT NOD
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Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	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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Chemische informatie, opslag en stabiliteit

Molecuulgewicht	207.25	Formule	C₁₀H₉NO₂S	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	19542-67-7	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	BAY 11-7821			Smiles	CC1=CC=C(C=C1)S(=O)(=O)C=CC#N

Oplosbaarheid

In vitro
Batch:

DMSO : 41 mg/mL (197.82 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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 formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

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 heft de NF-κB DNA-binding volledig en specifiek op, waardoor de NF-κB-induceerbare cytokine IL-6 wordt gedownreguleerd en apoptose wordt geïnduceerd. Deze verbinding (< 8 μM) is in staat om zowel de basale als de TNFα gestimuleerde NFκB luciferase-activiteit effectief te remmen op een dosisafhankelijke manier. Het (8 μM) remt sterk de proliferatiesnelheid in NCI-H1703 cellen. Deze verbinding (5 μM) vermindert snel en efficiënt de DNA-binding van NF-kappaB in HTLV-I-geïnfecteerde T-cellijnen en down-reguleert de expressie van het anti-apoptotische gen, Bcl-x(L), terwijl het weinig effect heeft op de DNA-binding van een andere transcriptiefactor, AP-1. Deze chemisch geïnduceerde apoptose van primaire ATL-cellen is prominenter dan die van normale perifere bloedmononucleaire cellen, en apoptose van deze cellen is ook geassocieerd met down-regulatie van NF-kappaB-activiteit. Het (5 μM) induceert selectief apoptose van HTLV-I-geïnfecteerde T-cellijnen geassocieerd met down-regulatie van de expressie van cycline D1, cycline D2 en Bcl-xL. Deze verbinding (100 μM) voorkomt de nucleaire translocatie van p65, uitgelokt door NMDA, en de NMDA-geïnduceerde toename van NF-κB-binding in muizen hippocampuscoupes. Het voorkomt NMDA-toxiciteit in het CA1-gebied van hippocampuscoupes met 40% neuroprotectie bij 20 μM en 70% neuroprotectie bij 100 μM. Deze chemische stof remt bij alle geteste concentraties significant de NF-κB p65 DNA-bindende activiteit in vetweefsel, terwijl het in skeletspieren, bij 50 μM en 100 μM, significant de NF-κB p65 DNA-bindende activiteit remt. Het (100 μM) vermindert IKK-β-eiwit in menselijk vetweefsel en skeletspieren. Deze verbinding (100 μM) vermindert significant de afgifte van TNF-α uit vetweefsel, terwijl de afgifte van IL-6 en IL-8 significant wordt geremd bij alle geteste concentraties van deze chemische stof. Het (50 μM) vermindert significant de afgifte van TNF-α, IL-6 en IL-8 in skeletspieren. Deze verbinding blijkt ook de E2-conjugerende enzymen Ubc (ubiquitine conjugerende) 13 en UbcH7 en de E3-ligase LUBAC (lineair ubiquitine-assemblagecomplex) te inactiveren, en induceert zo de dood van B-cellymfoom- en leukemische T-cellen.
In vivo	BAY 11-7082, een NF-κB-remmer, induceert apoptose en S-fase-arrest in maagkankercellen.
Referenties	[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/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	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

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