BAY-11-7082-BAY-11-7821-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBAY 11-7082Cat. No.: HY-13453CAS No.: 19542-67-7Synonyms: BAY 11-7821分式: CHNOS分量: 207.25作靶點: NF-B; IKK; Deubiquitinase; Autophagy; Apoptosis作通路: NF-B; Cell Cycle/DNA Damage; Autophagy; Apoptosis儲存式: Powder -20C 3 years4C 2 years

2、In solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (482.51 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 4.8251 mL 24.1255 mL 48.2509 mL5 mM 0.9650 mL 4.8251 mL 9.6502 mL10 mM 0.4825 mL 2.4125 mL 4.8251 mL請根據(jù)產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備

3、液的保存式和期限。體內實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結果的可靠性，體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (12.06 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (1

4、2.06 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 BAY 11-7082是NF-B 抑制劑， 其通過抑制TNF-誘導的IB-磷酸化來降低NF-B。 BAY 11-7082抑制泛素化蛋酶 USP7 和 USP21 的 IC50 分別為0.19 M 和 0.96 M。IC50 & Target NF-B USP7 USP21 Autophagy0.19 M (IC50) 0.96 M (IC50)體外研究 Bay 11-7082, an inhibitor

5、of NF-B, induces apoptosis of HTLV-I-infected T-cell lines but only negligibleapoptosis of HTLV-I-negative T cells. Bay 11-7082 rapidly and efficiently reduces the DNA binding of NF-Bin HTLV-I-infected T-cell lines and down-regulated the expression of the antiapoptotic gene, Bcl-xL, regulatedby NF-B

6、. Bay 11-7082 selectively inhibits Tax-induced NF-B activity in a human T-cell line 1. BAY 11-7082 inhibits NFB signalling and is recently shown to inhibit the majority of E2 and E3 ligases tested byreacting covalently with the catalytic cysteine residues. Moreover, BAY 11-7082 also inhibits several

7、 tyrosinephosphatases by reacting with catalytic Cys residue of these enzymes. NSC 697923 is originally shown toinhibit the E2 ligase Ubc13-Uev1A 2. BAY 11-7082 inhibits the phosphorylation of IB and activation ofNF-B, induces the death of HBL-1 cells. BAY 11-7082 completely suppresses the LPS-stimu

8、lated and IL-1-stimulated phosphorylation of the activation loop of IKK 3. BAY 11-7082 acts by inhibiting TNF-inducedphosphorylation of IB-, resulting in decreased NF-B and decreases expression of adhesion molecules 4.PROTOCOLKinase Assay 3 UBE1 (0.17 M) in 22.5 L of 20 mM Hepes, pH 7.5, containing

9、10 M ubiquitin is incubated for 45 min at21C with 1 L of DMSO or 1 L of BAY 11-7082 in DMSO. A 2.5 L solution of 10 mM magnesium acetateand 0.2 mM ATP is added, incubated for 10 min at 30C, and the reactions are terminated by the addition of2.5 L of 10% (w/v) SDS and heating for 6 min at 75C. The sa

10、mples are subjected to SDS/PAGE in theabsence of any thiol. The gels are stained for 1 h with Coomassie Instant Blue and destained by washingwith water. The loading of ubiquitin to E2 conjugating enzymes is carried out in an identical manner, exceptthat UBE1 (0.17 M) is mixed with Ubc13 (2.4 M) or U

11、bcH7 (2.9 M) prior to incubation with BAY 11-70823.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 The effect of Bay 11-7082 on cell growth is assayed by the WST-1 method. 2104 (cell lines) or 2105(PBMCs) cells are incubated in a 96-well mi

12、croculture plate under the above conditions in the absence orpresence of various concentrations of Bay 11-7082 (1, 2, 3, 4, and 5 M). After 48 hours of culture, 10 LWST-1 solution is added and the cells are further incubated for another 2 hours. The number of survivingcells is measured with a microp

13、late reader at a reference wavelength of 655 nm and test wavelength of 450nm. Cell viability is determined as percentage of the control (ie, absence of Bay 11-7082) 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發(fā)表的科研獻2/3 Master of Small Molecul

14、es 您邊的抑制劑師www.MedChemE Gut. 2018 Nov;67(11):2035-2044. J Immunother Cancer. 2019 Jul 12;7(1):178. Cell Mol Life Sci. 2018 Jul;75(14):2627-2641. Cell Mol Life Sci. 2018 Mar;75(6):1117-1132. Br J Pharmacol. 2019 Jun;176(11):1717-1727.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1

15、. Mori N, et al. Bay 11-7082 inhibits transcription factor NF-kappaB and induces apoptosis of HTLV-I-infected T-cell lines andprimary adultT-cell leukemia cells. Blood. 2002 Sep 1;100(5):1828-1834.2. Ritorto MS, et al. Screening of DUB activity and specificity by MALDI-TOF mass spectrometry. Nat Com

16、mun. 2014 Aug 27;5:4763.3. Strickson S, et al. The anti-inflammatory drug BAY 11-7082 suppresses the MyD88-dependent signalling network by targeting theubiquitin system. Biochem J. 2013 May 1;451(3):427-437.4. Pierce JW, et al. Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesion molecule expressionshow anti-inflammatory effects in vivo.