GLPBio

MZP-54

Catalog No.: GC33102Purity:>98.00%
COASDSData Sheet
MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 4 nM for Brd4BD2.

Products are for research use only. Not for human use. We do not sell to patients.

MZP-54
Cas No.: 2010159-47-2
10mM (in 1mL DMSO)In Stock
$891.00
1
5mgIn Stock
$506.00
1
10mgIn Stock
$782.00
1
25mgIn Stock
$1,471.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

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Description

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.

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].

[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.

Protocol

Cell experiment:

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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
2010159-47-2
SMILES
O=C(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N1C[C@H](O)C[C@H]1C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O)C(C=C4)=CC=C4C5=CC6=C(C=C5)N(C(C)=O)[C@@H](C)C[C@H]6NC7=CC=C(Cl)C=C7
Molecular Formula
C55H66ClN7O9S
Molecular Weight
1036.67
Solubility
Ethanol : 50 mg/mL (48.23 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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