BAY 11-7082

Catalog No.S2913

BAY 11-7082 is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. Also inhibiting components of the ubiquitin system.

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BAY 11-7082 Chemical Structure

BAY 11-7082 Chemical Structure
Molecular Weight: 207.25

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Related Compound Libraries

BAY 11-7082 is available in the following compound libraries:

IκB/IKK Inhibitors with Unique Features

  • Pan IKK Inhibitor

    IKK-16 (IKK Inhibitor VII) Pan-IKK inhibitor, IKK-2, IC50=40 nM; IKK-1, IC50=200 nM.

  • Most Potent IKK Inhibitor

    TPCA-1 IKK-2, IC50=17.9 nM.

  • IKK Inhibitor in Clinical Trial

    Bardoxolone Methyl Phase III for Chronic Kidney Disease and Type 2 Diabetes.

  • Newest IKK Inhibitor

    Bay 11-7085 Irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.

Product Information

  • Compare IκB/IKK Inhibitors
    Compare IκB/IKK Products
  • Research Area

Product Description

Biological Activity

Description BAY 11-7082 is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. Also inhibiting components of the ubiquitin system.
Targets E2-conjugating enzymes [6]
(Cell-free assay)
IκBα phosphorylation [1]
(Tumor cells)
IC50 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. [1] BAY 11-7082 (< 8 μM) is able to effectively inhibit both basal and TNFα stimulated NFκB luciferase activity in a dose dependent manner. BAY 11-7082 (8 μM) strongly inhibits the rate of proliferation in NCI-H1703 cells. [2] Bay 11-7082 (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. Bay 11-7082-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. Bay 11-7082 (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. [3] BAY 11-7082 (100 μM) prevents the nuclear translocation of p65 elicited by NMDA and the NMDA-induced increase of NF-κB binding in mouse hippocampal slices. BAY 11-7082 prevents NMDA toxicity occurring in CA1 region of hippocampal slices with 40% neuroprotection at 20 μM and 70% neuroprotection at 100 μM. [4] BAY 11-7082 at all concentrations tested significantly inhibits NF-κB p65 DNA-binding activity in adipose tissue, whereas in skeletal muscle, BAY 11-7082 at 50 μM and 100 μM significantly inhibits NF-κB p65 DNA-binding activity. BAY 11-7082 (100 μM) reduces IKK-β protein in human adipose tissue and skeletal muscle. BAY 11-7082 (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 BAY 11-7082 tested. BAY 11-7082 (50 μM) significantly decreases the release of TNF-α, IL-6, and IL-8 in skeletal muscle. [5] BAY 11-7082 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. [6]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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RAW 264.7NWjTWmdkTnWwY4Tpc44hSXO|YYm=NVWwS2hLOi1zNTFOwG0>M2XDWFEhcA>?NVHYdnpnTE2VTx?=NF7YWIh{fXCycnXzd4V{KHSqZTDhZ5RqfmG2aX;uJI9nKEmNSzDmZY1qdHlibXXtZoVzew>?NWnpd4xVOjN2NEG3N|A>
IL-1R MoL4SpVv[3Srb36gRZN{[Xl?NI\5cHozNTF3IN88US=>M1Pi[FEhcA>?NIexbmFFVVORMn61d5VxeHKnc4Pld{B1cGViYXP0bZZifGmxbjDv[kBKU0tiZnHtbYx6KG2nbXLldpM>NHjG[FEzOzR2MUezNC=>
RAW 264.7MlHjSpVv[3Srb36gRZN{[Xl?NX32SHRXOTVizszNNHm2cJkyKGh?NEXhd3hFVVORM{XQUJN2eHC{ZYPz[ZMhfGinIHHjeIl3[XSrb36gc4Yh[W6mIFrOTy=>MojzNlM1PDF5M{C=
IL-1R MoHZSpVv[3Srb36gRZN{[Xl?MUexOUDPxE1?M4e3SFEhcA>?NInub3pFVVORMXPzeZBxemW|c3XzJJRp\SCjY4TpeoF1cW:wIH;mJIFv\CCMTlu=MkTiNlM1PDF5M{C=
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MT‐1 MXHGeY5kfGmxbjDBd5NigQ>?NYCwZnNxQMLiwsXtMVqzJIg>MnLL[IVkemWjc3XzJJRp\SCuZY\lcJMhd2ZicPMAlHNVSVR|IHHu[EBx6oDSNFXCVFE>Mo\NNlMzPzh2N{m=
MT‐2 M4\uSmZ2dmO2aX;uJGF{e2G7M2PubljDqML3bR?=MVSzJIg>MnrR[IVkemWjc3XzJJRp\SCuZY\lcJMhd2ZicPMAlHNVSVR|IHHu[EBx6oDSNFXCVFE>M37tPFI{Ojd6NEe5
MT‐1 NYnud4VSTnWwY4Tpc44hSXO|YYm=NFntRog5yqEEtX2=NE\qfpc{KGh?NEPXUYpl\WO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUheDZ3IIP1ZpVvcXRib3[gUmbjiJEQulNCpC=>M3P1e|I{Ojd6NEe5
MT‐2 M4qzcWZ2dmO2aX;uJGF{e2G7MmHuPOKhyrWvMnjTN{BpM3LtcoRm[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBxPjVic4XieY5qfCCxZjDOSwKBmM78QtMgNXL5c3k4OjN{N{i0O|k>
MCF-7 MmqwSpVv[3Srb36gRZN{[Xl?MV:yMlUuOTVizszNMmfTNE42KGh?NE\OTHVFVVORMnXzZ4F2e2W|IITo[UBoemGmdXHsJIxwe3Nib3[gZ4VtdCCjZHjld4lwdg>?NEPrbWIzOzB7M{KyOy=>
HaCaT MYjGeY5kfGmxbjDBd5NigQ>?MnvlOU4xyqEQvF2=M3vrPFHDqGkEoB?=NWPoNGFY[XS2ZX71ZZRmeyC2aHWgWGNQUC2rbnT1Z4VlKHC{b3T1Z5Rqd25ib3[gTWwuPsLiMnmwNlMxPDFzNki=
A549 MU\GeY5kfGmxbjDBd5NigQ>?MUixJIg>MUDpcohq[mm2czDMWGEucW6mdXPl[EBUWC2DIH3SUmEheHKxZIXjeIlwdsLic3nncolncWOjboTsfS=>NXTzRYZ4OjNyM{GyNVM>
OA chondrocytes MnTFSpVv[3Srb36gRZN{[Xl?NXPZdoZDOTBizszNNVjCc2Y5OSCqMl7HZoxw[2u|IITo[UBCT0VvQmPBMYlv\HWlZXSg[4Vv\S:ycn;0[YlvKGW6cILld5Nqd25ib3[gS3JRPzhib4KgR29ZNTJiKIC8NE4xPSl?M17KRVIzQTh{MkK4
RAW264.7NWD6VGg{TnWwY4Tpc44hSXO|YYm=NXPkSndmOTVizszNNEPVOpoyPS1zMkCgcYlvMUHicI9kc3NidHjlJJBzd2S3Y4Tpc44hd2ZiTl:sJHBITTJuIHHu[EBVVkZvzsG=NIq0bI0zOjd2NUWyNy=>
RAW264.7Ml2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYTPOYUxPS1|MDFOwG0>NXTZcVlHOjRiaB?=MV;pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>MknPNlI4PDV3MkO=
HBL6MmPZRZBweHSxc3nzJGF{e2G7NXnMdIhJOC53L{WvNlUh|ryPMYq2M|I1KGh?NWfwOlZ[\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIFv\CCuZXXh[JMhfG9iYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC=M1r2[FIzODd2OEKw
HT29 NFLzb4tHfW6ldHnvckBCe3OjeR?=NWflVVI{OS1zMDFOwG0>MVWxNOKhcA>?NFH3W3VqdmO{ZXHz[ZMhUE9vMTDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36=MXmyNVYzODl4NB?=
Ca9–22NIGwS2dCeG:ydH;zbZMhSXO|YYm=Mom3NVDDqM7:TdMgNFfrSmcyKGh?MlnuZ49ueGyndHXsfUBqdmirYnn0d{BCVEFvUFTUMYlv\HWlZXSgZZBweHSxc3nzNEn1NW8zOTF|OES4NC=>
Ca9–22MWrGeY5kfGmxbjDBd5NigQ>?M4PSelExyqEQvF5CpC=>M1TzbVEhcA>?NHvSW4dkd22ybHX0[Yx6KGGkcn;nZZRmeyC2aHWgRWxCNVCGVD3pcoR2[2WmIFrOT{Bi[3SrdnH0bY9vNYHIRmlZOjFzM{i0PFA>
A-549M2DBWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXKxNOKh|ryPwrC=MViyOE81QCCqM2i4SIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGgeIlu\S2mZYDlcoRmdnRibXHucoVzNI\seYYzODh4NkC0Ny=>
APNYriUFlHTnWwY4Tpc44hSXO|YYm=NVvHVGNQPS9zMDFOwG0>NXHWdVRiPDhiaB?=NWjZNXFb\G:5boLl[5Vt[XSnczD0bIUhSkGGIIDyc5RmcW5ibHX2[Ywh[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=M2PLelIxPTl4NkS1
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AQ1MnTMSpVv[3Srb36gRZN{[Xl?Mlq3NlAh|ryPNVTMNJNUPC96IHi=MmS2[I94dnKnZ4XsZZRmeyC2aHWgRmFFKHC{b4TlbY4hdGW4ZXygZUB1cW2nLXTldIVv\GWwdDDtZY5v\XJ?MVmyNFU6PjZ2NR?=
THP-1M4DEV2Z2dmO2aX;uJGF{e2G7NGDNU3U2yqEQvF5CpC=>M2rGTlAvPSCqNHz6V5lifHSnboXheIV{KHSqZTDMVHMucW6mdXPl[EBxNUoQulNOtUBxem:2ZXnuJIJ6KDd{JR?=NF36dYozODNyOUexPC=>
K562NIrwWVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NX;ZOHViOi1|MDFOwG0>MYGyOEBpM4nScGlEPTB;ODFOwG0tcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?MUOxPVY1PjhyNx?=
JurketMl[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkmyNk0{OCEQvF2=M{\aVVI1KGh?NIS5U4xKSzVyPUeuNUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyNVW5XXp1OTl4NE[4NFc>
U937NVXoTnBST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NVPqXpVWOi1|MDFOwG0>MmjhNlQhcA>?M3nreWlEPTB;MUCuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyM3Wx[|E6PjR4OEC3
PBMCM4rFZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MYSyMVMxKM7:TR?=MXiyOEBpMlnkTWM2OD12MD6yJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=MlHmNVk3PDZ6MEe=
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... Click to View More Cell Line Experimental Data

In vivo
Features

Protocol(Only for Reference)

Cell Assay: [2]

Cell lines NCI-H1703 cells
Concentrations ~8 μM
Incubation Time 12 hours
Method Cells are transfected with siRNA in 96-well microtiter plates and then cultured for 72 hours in complete NSCLC medium, treated with BAY 11-7082 for 12 hours. Cells are incubated with [3H]thymidine for 3 hours. The cells are collected on filters using an automatic cell harvester and radioactivity on the filters is measured by β-scintillation counting.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Melisi D, et al. Expert Opin Ther Targets, 2007, 11(2), 133-144.

[2] Gastonguay A, et al. Cancer Biol Ther, 2012, 13(8), 647-656.

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Chemical Information

Download BAY 11-7082 SDF Download BAY 11-7082 SDF
Molecular Weight (MW) 207.25
Formula

C10H9NO2S

CAS No. 19542-67-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms BAY 11-7821
Solubility (25°C) * In vitro DMSO 41 mg/mL (197.82 mM)
Ethanol 10 mg/mL (48.25 mM)
Water <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 15 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-Propenenitrile, 3-[(4-methylphenyl)sulfonyl]-, (2E)-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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