Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
Other Sizes |
|
Purity: ≥98%
BAY 11-7082 (BAY-11-7082; BAY-117082) is a novel and potent NF-κB inhibitor with potential anti-inflammatory and anticancer activity. In tumor cells, it has an IC50 of 10 M and prevents TNFα from causing IB phosphorylation.
Targets |
USP7 (IC50 = 0.19 μM); USP21(IC50 = 0.96 μM); Autophagy; NF-κB
|
---|---|
ln 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) can effectively inhibit NF-κB luciferase activity at both basal and TNFα -stimulated levels in a dose-dependent manner. The rate of proliferation in NCI-H1703 cells is significantly inhibited by BAY 11-7082 (8 μM).[2] Bay 11-7082 (5 μM) has little impact on the DNA binding of another transcription factor, AP-1, it rapidly and effectively decreases the DNA binding of NF-kappaB in HTLV-I-infected T-cell lines and downregulates the expression of the antiapoptotic gene Bcl-x(L). BPrimary ATL cells are more susceptible to the apoptosis caused by Bay 11-7082 than are healthy peripheral blood mononuclear cells, and this apoptosis is also accompanied by a down-regulation of NF-kappaB activity. With the expression of cyclin D1, cyclin D2, and Bcl-xL being downregulated, Bay 11-7082 (5 μM) specifically causes apoptosis in HTLV-I-infected T-cell lines.[3] In mouse hippocampal slices, BAY 11-7082 (100 μM) inhibits the nuclear translocation of p65 induced by NMDA as well as the NMDA-induced rise in NF-κB binding. With 40% neuroprotection at 20 μM and 70% neuroprotection at 100 M, BAY 11-7082 inhibits NMDA toxicity in the CA1 region of hippocampal slices.[4] In adipose tissue, BAY 11-7082 significantly inhibits NF-κB p65 DNA-binding activity at all tested concentrations, whereas BAY 11-7082 significantly inhibits NF-κB p65 DNA-binding activity in skeletal muscle at 50 μM and 100 μM. Human adipose tissue and skeletal muscle IKK-βprotein levels are decreased by BAY 11-7082 (100 μM). TNF-release from adipose tissue is significantly reduced by BAY 11-7082 (100 μM), whereas the release of IL-6 and IL-8 is significantly inhibited at all BAY 11-7082 concentrations tested. The skeletal muscle release of TNF-α, IL-6, and IL-8 is markedly reduced by BAY 11-7082 (50 μM). [5] |
ln Vivo |
In gastric cancer cells, BAY 11-7082, an NF-B inhibitor, causes apoptosis and S phase arrest.
|
Enzyme Assay |
UBE1 (0.17 μM) in 22.5 μL of 20 mM Hepes, pH 7.5, containing 10 μM ubiquitin is incubated for 45 min at 21°C with 1 μL of DMSO or 1 μL of BAY 11-7082 in DMSO. A 2.5 μL solution of 10 mM magnesium acetate and 0.2 mM ATP is added, incubated for 10 min at 30°C, and the reactions are terminated by the addition of 2.5 μL of 10% (w/v) SDS and heating for 6 min at 75°C. The samples are subjected to SDS/PAGE in the absence of any thiol. The gels are stained for 1 h with Coomassie Instant Blue and destained by washing with water. The loading of ubiquitin to E2 conjugating enzymes is carried out in an identical manner, except that UBE1 (0.17 μM) is mixed with Ubc13 (2.4 μM) or UbcH7 (2.9 μM) prior to incubation with BAY 11-7082.
|
Cell Assay |
In 96-well microtiter plates, siRNA is transfected into the cells, which are then cultured for 72 hours in complete NSCLC medium and given a 12-hour BAY 11-7082 treatment. Three hours are spent incubating the cells with [3H]thymidine. The radioactivity on the filters is determined by β-scintillation counting after the cells are collected on filters using an automatic cell harvester.
|
Animal Protocol |
Male BALB/c nude mice.
2.5 & 5 mg/kg i.t. |
References |
[1]. Expert Opin Ther Targets . 2007 Feb;11(2):133-44. [2]. Cancer Biol Ther . 2012 Jun;13(8):647-56. [3]. J Med Chem . 2005 Sep 22;48(19):5966-79. [4]. J Med ChemBlood . 2002 Sep 1;100(5):1828-34. [5]. Neurosci Lett . 2005 Apr 4;377(3):147-51. [6]. iochem J . 2013 May 1;451(3):427-37. |
Molecular Formula |
C10H9NO2S
|
---|---|
Molecular Weight |
207.25
|
Exact Mass |
207.04
|
Elemental Analysis |
C, 57.96; H, 4.38; N, 6.76; O, 15.44; S, 15.47
|
CAS # |
19542-67-7
|
Appearance |
Solid powder
|
SMILES |
CC1=CC=C(C=C1)S(=O)(=O)/C=C/C#N
|
InChi Key |
DOEWDSDBFRHVAP-KRXBUXKQSA-N
|
InChi Code |
InChI=1S/C10H9NO2S/c1-9-3-5-10(6-4-9)14(12,13)8-2-7-11/h2-6,8H,1H3/b8-2+
|
Chemical Name |
(E)-3-(4-methylphenyl)sulfonylprop-2-enenitrile
|
Synonyms |
BAY 11-7821; BAY-11-7821; BAY11-7821; BAY 11-7082; BAY11-7082; BAY 117082; BAY117082; BAY-117082; BAY-11-7082
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.8251 mL | 24.1255 mL | 48.2509 mL | |
5 mM | 0.9650 mL | 4.8251 mL | 9.6502 mL | |
10 mM | 0.4825 mL | 2.4125 mL | 4.8251 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
BAY 11-7082 suppresses the activation of IKK family members and JNK.Biochem J. 2013 May 1;451(3):427-437. th> |
---|
BAY 11-7082 does not affect the LPS-stimulated autophosphorylation of IRAK4. BAY 11-7082 suppresses the LPS- or IL-1-stimulated formation of K63-pUb chains and the DNA damage response.Biochem J. 2013 May 1;451(3):427-437. td> |