MZP-54 - PROTAC - 生命科學(xué)試劑 - 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作靶點(diǎn): PROTAC; Epigenetic Reader Domain作通路: PROTAC; Epigenetics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) Ethanol : 50 mg/mL

2、(48.23 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使

3、；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.41 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% EtOH 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (2.41 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% EtOH 90% corn oilSolubility: 2.5 mg

4、/mL (2.41 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 MZP-54于 PROTAC 技術(shù)的種選擇性的 BRD3/4 降解劑，對(duì) Brd4BD2 的 Kd 值為 4 nM。IC50 & Target Kd: 4 nM (Brd4BD2) 1體外研究 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