2010159-48-3

2010159-48-3 structure

Name: MZP-55
Chemical Name: MZP-55
CAS Number: 2010159-48-3
Molecular Formula: C₅₇H₇₀ClN₇O₁₀S
Molecular Weight: 1080.72
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2018-09-09 07:20:46
Modify Date: 2024-01-10 16:15:13
MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2.

Name	MZP-55

Description	MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2.
Related Catalog	Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain Signaling Pathways >> PROTAC >> PROTAC Research Areas >> Cancer
Target	Kd: 8 nM (Brd4BD2)[1]
In Vitro	MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2. MZP-55 binds to VHL-EloC-EloB protein (VCB) with a Kd of 105 ± 24 nM. MZP-55 shows an inhibitory activity against MV4;11 and HL60 cells, with pEC50s of 7.31 ± 0.03 and 6.57 ± 0.02, respectively[1].
Cell Assay	MV4;11 or HL60 cells are incubated with MZP-55 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-55 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-55[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.