CeMMEC13-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECeMMEC13Cat. No.: HY-101088CAS No.: 1790895-25-8分式: CHNO分量: 336.34作靶点: DNA/RNA Synthesis作通路: Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 30 mg/mL (89.20 mM)* means

2、soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9732 mL 14.8659 mL 29.7318 mL5 mM 0.5946 mL 2.9732 mL 5.9464 mL10 mM 0.2973 mL 1.4866 mL 2.9732 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 CeMMEC13种有效的 TAF1 (2) 抑制剂，IC50 值为 2.1 M。IC50 & Tar

3、get IC50: 2.1 M (TAF1 (2) 1体外研究CeMMEC13 is a potent inhibitor of TAF1 (2) bromodomain, with an IC50 of 2.1 M. CeMMEC13 shows littleor no effects on REDNESS, BRD4, CREBBP. CeMMEC13 (0-20 M) in combination with (S)-JQ1 increases1/2 Master of Small Molecules 您边的抑制剂师www.MedChemERFP expression in REDS3 c

4、ells and is effective reducing the viability of H23 and THP1 cells, better than thatof single treatment 1.PROTOCOLKinase Assay 1 TAF1 binding assays are conducted using the EPIgeneous Binding Domain kit B. Binding is determined bythe displacement of an acetylated biotin peptide from a GST-tagged TAF

5、1 protein using HTRF with a Eu3+-conjugated GST antibody donor and streptavidin-conjugated acceptor. Compounds (CeMMEC13) aredispensed into assay plates, ProxiPlate-384 Plus using an Echo 525 Liquid Handler. Binding assays areconducted in a final volume of 20 L with 5 nM TAF1-GST, 50 nM peptide (SGR

6、GK (ac)GGK (ac)GLGK(ac)GGAK (ac)RHRK (biotin)-acid), 6.25 nM Streptavidin-XL665, 1:200 Anti-GST-Eu3+ cryptate and 0.1%DMSO. Assay reagents are dispensed into plates using a Multidrop combi and incubated at roomtemperature for 3 h. Fluorescence is measured using a PHERAstar microplate reader using th

7、e HTRFmodule with dual emission protocol (A = excitation of 320 nm, emmission of 665 nm, and B = excitation of320 nm, emission of 620 nm). Raw data are processed to give an HTRF ratio (channel A/B 10,000), whichis used to generate IC50 curves 1.MCE has not independently confirmed the accuracy of the

8、se methods. They are for reference only.Cell Assay 1 Cells are seeded on clear flat-bottom 96-well or 384-well plates and treated with the indicated compounds(CeMMEC13) for the specified conditions. Live-cell imaging pictures are taken with the Operetta HighContent Screening System, 20 objective and

9、 nonconfocal mode 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Sdelci S, et al. Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk. Nat Chem Biol. 2016Jul;12(7):504-10.McePdfHeightCaution: Product has not been fully validated for medica