2010159-47-2

2010159-47-2 structure

Name: MZP-54
Chemical Name: MZP-54
CAS Number: 2010159-47-2
Molecular Formula: C₅₅H₆₆ClN₇O₉S
Molecular Weight: 1036.67
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2018-08-21 07:23:15
Modify Date: 2024-01-04 16:22:07
MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.

Name	MZP-54

Description	MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.
Related Catalog	Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain Signaling Pathways >> PROTAC >> PROTAC Research Areas >> Cancer
Target	Kd: 4 nM (Brd4BD2)[1]
In Vitro	MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2. MZP-54 binds to VHL-EloC-EloB protein (VCB) with a Kd of 105 ± 24 nM. MZP-54 shows an inhibitory activity against MV4;11 and HL60 cells, with pEC50s of 7.08 ± 0.05 and 6.37 ± 0.03, respectively. MZP-54 also exhibits high depletion of cMyc levels[1].
Cell Assay	MV4;11 or HL60 cells are incubated with MZP-54 at the desired concentration for 48 h on a clear-bottom 384-well plate. Cells are kept in RPMI medium supplemented with 10% FBS, l-glutamine, penicillin, and streptomycin. Initial cell density is 3 × 105 per mL. Cells are treated with various concentrations of MZP-54 or 0.05% DMSO. After treatment, cell viability is measured with cell viability assay kit. Signal is recorded. Data are analyzed with Graphpad Prism software to obtain EC50 values of each MZP-54[1].
References	[1]. Chan KH, et al. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513.