CeMMEC1 - Epigenetic Reader Domain 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECeMMEC1Cat. No.: HY-111445CAS No.: 440662-09-9分式: CHNO分量: 336.34作靶點(diǎn): Epigenetic Reader Domain; DNA/RNA Synthesis作通路: Epigenetics; Cell Cycle/DNA Damage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

2、實(shí)驗(yàn) DMSO : 100 mg/mL (297.32 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 CeMMEC1BRD4 的抑制劑，同時(shí)對(duì) TAF1 有很的親和性，對(duì)

3、 TAF1 的 IC50 值為 0.9 M，對(duì) TAF1 (2) 的Kd 值為 1.8 M。IC50 & Target Kd: 1.8 M (TAF1 (2) 1IC50: 0.9 M (TAF1) 1體外研究CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 M for TAF1, and1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEa Kd of 1.8 M for TAF1 (2) and slso shows

4、 high affinity for the bromodomains of CREBBP, EP300, BRD9.CeMMEC1 (1, 10, 20 M) decreases the number of THP1 cells in S phase in a dose manner. CeMMEC1also induces apoptosis. CeMMEC1 in combination with (S)-JQ1 displays potently impaired cell viability thantreatment alone 1.PROTOCOLKinase Assay 1 T

5、AF1 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 TAF1 protein using HTRF with a Eu3+-conjugated GST antibody donor and streptavidin-conjugated acceptor. Compounds (CeMMEC1) aredispen

6、sed 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 (SGRGK (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 r

7、eagents are dispensed into plates using a Multidrop combi and incubated at roomtemperature for 3 h. Fluorescence is measured using a PHERAstar microplate reader using the HTRFmodule with dual emission protocol (A = excitation of 320 nm, emmission of 665 nm, and B = excitation of320 nm, emission of 6

8、20 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 these methods. They are for reference only.Cell Assay 1 Cells are seeded on clear flat-bottom 96-well or 384-well plates and treated w

9、ith the indicated compounds(CeMMEC1) for the specified conditions. Live-cell imaging pictures are taken with the Operetta High ContentScreening System, 20 objective and 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 fo