MZP-54 - PROTAC - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMZP-54Cat. No.: HY-112376CAS No.: 2010159-47-2分式: CHClNOS分量: 1036.67作靶点: PROTAC; Epigenetic Reader Domain作通路: PROTAC; Epigenetics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 Ethanol : 50 mg/mL

2、(48.23 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.9646 mL 4.8231 mL 9.6463 mL5 mM 0.1929 mL 0.9646 mL 1.9293 mL10 mM 0.0965 mL 0.4823 mL 0.9646 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。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使

3、；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.41 mM); Clear solution2. 请依序添加每种溶剂： 10% EtOH 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (2.41 mM); Clear solution3. 请依序添加每种溶剂： 10% EtOH 90% corn oilSolubility: 2.5 mg

4、/mL (2.41 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 MZP-54于 PROTAC 技术的种选择性的 BRD3/4 降解剂，对 Brd4BD2 的 Kd 值为 4 nM。IC50 & Target Kd: 4 nM (Brd4BD2) 1体外研究 MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.MZP

5、-54 binds to VHL-EloC-EloB protein (VCB) with a Kd of 105 24 nM. MZP-54 shows an inhibitoryactivity against MV4;11 and HL60 cells, with pEC50s of 7.08 0.05 and 6.37 0.03, respectively. MZP-54also exhibits high depletion of cMyc levels 1.PROTOCOLCell Assay 1 MV4;11 or HL60 cells are incubated with MZ

6、P-54 at the desired concentration for 48 h on a clear-bottom384-well plate. Cells are kept in RPMI medium supplemented with 10% FBS, l-glutamine, penicillin, andstreptomycin. Initial cell density is 3 105 per mL. Cells are treated with various concentrations of MZP-54 or0.05% DMSO. After treatment,

7、cell viability is measured with cell viability assay kit. Signal is recorded. Dataare analyzed with Graphpad Prism software to obtain EC50 values of each MZP-54 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Chan KH, et al. Impact of Tar

8、get Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain andExtra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J MedChem. 2018 Jan 25;61(2):504-513.McePdfHeightCaution: Product has not been fully validated for medical applications.F