1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECU-CPT22Cat. No.: HY-108471CAS No.: 1416324-85-0分式: CHO分量: 362.37作靶點: Toll-like Receptor (TLR)作通路: Immunology/Inflammation儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (344.95 m

2、M)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.90 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.90 mM); Suspended solution; Need ultrasonic1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility:

3、 2.5 mg/mL (6.90 mM); Suspended solution; Need ultrasonicBIOLOGICAL ACTIVITY物活性 CU-CPT22種 toll 樣受體 1 和 2 (TLR1/2) 抑制劑， 其 IC50 值為 0.58 M。IC50 & Target IC50: 0.58 M (TLR1/2) 1體外研究 CU-CPT22 is a toll-like receptor 1 and 2 (TLR1/2) inhibitor with an IC50 of 0.580.09 M. It is demonstratedthat CU-CPT22 is

4、 able to compete with Pam3CSK4 for binding to TLR1/2 with an inhibition constant (Ki) of0.410.07 M, which is consistent with its potency observed in the whole cell assay. Increasing theconcentration of CU-CPT22 to 6 M decreases the anisotropy to background levels. It is found that CU-CPT22 inhibits

5、TLR1/2 signaling without affecting other TLRs, showing it is highly selective in intact cells.CU-CPT22 is found to have no significant cytotoxicity at various concentrations up to 100 M in RAW 264.7cells. The result demonstrates that CU-CPT22 can inhibit about 60% of TNF-and 95% of IL-1 at 8 M 1.PRO

6、TOCOLKinase Assay 1 RAW 264.7 cells are planted in 6-well plates at 1,000,000 cells per well with 3 mL of medium and grown for24 h at 37C in a 5% CO2 humidified incubator. After 24 h, non-adherent cells and media are removed andreplaced with fresh RPMI 1640 medium (3 mL/well). Two wells of adherent

7、macrophages are treated withPam3CSK4 (300 ng/mL) as the positive control, two wells are treated with 8 M CU-CPT22, and the othertwo wells are treated with 8 M compound DMSO. Plates are then incubated for an additional 24 h. Themedium is removed, the cells are washed with PBS (31 mL), the plate is pu

8、t on ice, then 500 L of lysisbuffer is added to each well. The production of the cytokine interleukin-1 (IL-1) and TNF- is quantifiedwith enzyme-linked immunosorbent assays (ELISA). The cytokine level in each sample is determined induplicate 1.MCE has not independently confirmed the accuracy of thes

9、e methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Oxid Med Cell Longev. 2019 Apr. Life Sci. 2019 May 1;224:212-221.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Cheng K, et al. Discovery of small-molecule inhibitors of the TLR1/TLR2 complex. Angew Chem Int Ed Engl. 2012 Dec 3;51(49):12246-9.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution: Product has not been fully validated for me