NG25 _TAK1 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENG25Cat. No.: HY-15434CAS No.: 1315355-93-1分式: CHFNO分量: 537.58作靶點(diǎn): MAP4K; MAP3K作通路: MAPK/ERK Pathway儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (186.02 mM)H2O : 40% PEG300 5%

2、Tween-80 45% salineSolubility: 2.5 mg/mL (4.65 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.65 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 NG25種 TAK1 和 MAP4K2 的雙抑制劑，IC50 值分別為 149 nM 和 21.7 nM。IC50 & Target MAP4K2 TAK1 L

3、YN GSK21.7 nM (IC50) 149 nM (IC50) 12.9 nM (IC50) 56.4 nM (IC50)ABL,ARG FER SRC Eph B275.2 nM (IC50) 82.3 nM (IC50) 113 nM (IC50) 672 nM (IC50)ZAK Eph A2 Eph B4 ZC1/HGK698 nM (IC50) 773 nM (IC50) 999 nM (IC50) 3250 nM (IC50)RAF17590 nM (IC50)體外研究 NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with

4、 IC50s of 149 nM and 21.7 nM, respectively. NG25also potently suppresses several kinases such as LYN, CSK, FER, p38, ABL,ARG and SRC, with IC50s of12.9, 56.4, 82.3, 102, 75.2, and 113 nM, respectively 1. NG25 is very potent suppressor of CpG B- or CpGA-stimulated secretion of IFN and CL097-stimulate

5、d secretion of IFN, with complete inhibition by 400 nM2. NG25 treatment reduces cell viability of all tested breast cancer cell lines in a dose dependent manner.NG25 (2M) enhances the cytotoxic effect of Dox on breast cancer cells 3.PROTOCOLKinase Assay 2 IRF7 is expressed in Escherichia coli as a g

6、lutathione S-transferase (GST) fusion protein with a PreScissionproteinase cleavage site between the GST and the IRF7. The GST-IRF7 is captured on glutathione-Sepharose and IRF7 released from GST and glutathione-Sepharose by digestion with PreScissionproteinase. His6-tagged IKK and TBK1 are expresse

7、d in their active phosphorylated forms in insect Sf21cells and purified by affinity chromatography on nickel nitrilotriacetate-agarose. Active GST-IKK ispurchased from Millipore and assayed.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 2 3.

8、5105 Gen2.2 cells or Flt3-DCs are incubated for 1 h in 96-well plates without or with the indicatedconcentrations of inhibitor, then stimulated with 1 M CpG (type A or B) or 1 g/mL of CL097 or R848. After 5or 12 h the cell culture supernatants are collected, clarified by centrifugation, and frozen a

9、t 80C untilcytokine levels are analyzed. For cell viability assays, unstimulated cells are incubated for 12 h in theabsence or presence of inhibitors. Cells are then fixed and the percentage of live cells analyzed by flowcytometry.MCE has not independently confirmed the accuracy of these methods. Th

10、ey are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn)2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Nat Cell Biol. 2017 Oct;19(10):1248-1259. J Cell Biol. 2018 Aug 6;217(8):2727-2742. Cell Death Differ. 2019 Mar 8. Oncogene. 2017 Oct 5;36(40):5620-5630. Sci Signal. 2018 Jul 10;11(538). pii: eaan5850.See more cus

11、tomer validations on HYPERLINK / www.MedChemEREFERENCES1. Tan L, et al. Discovery of type II inhibitors of TGF-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase2 (MAP4K2). J Med Chem. 2015 Jan 8;58(1):183-96.2. Pauls E, et al. Essential role for IKK in production of type 1 interferons by plasmacytoid dendritic cells. J Biol Chem. 2012 Jun1;287(23):19216-28.3. Wang Z, et al. TAK1 inhibitor NG25 enhances doxorubicin-mediated apoptosis in breast cancer cells. Sci Rep. 2016 Sep 7;6:32737.McePdfHeightCaution: Produ