Name: MZP-55
Brand: BOC Sciences
Rating: 5 (1 reviews)

Size

Price

Stock

Quantity

$--

In stock

Solubility

Soluble in DMSO

Storage

Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping

Room temperature in continental US; may vary elsewhere

Synonyms

MZP-55; MZP 55; MZP55; (2S,4R)-1-[(2S)-2-[[2-[2-[2-[2-[2-[[4-[(2S,4R)-1-acetyl-4-(4-chloroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoyl]amino]ethoxy]ethoxy]ethoxy]ethoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide

InChI Key

UHWNJFZTYJNBAN-HYXXSBGTSA-N

InChI

InChI=1S/C57H70ClN7O10S/c1-36-29-48(62-45-18-16-44(58)17-19-45)47-30-43(15-20-49(47)65(36)38(3)66)40-11-13-42(14-12-40)54(69)59-21-22-72-23-24-73-25-26-74-27-28-75-34-51(68)63-53(57(4,5)6)56(71)64-33-46(67)31-50(64)55(70)60-32-39-7-9-41(10-8-39)52-37(2)61-35-76-52/h7-20,30,35-36,46,48,50,53,62,67H,21-29,31-34H2,1-6H3,(H,59,69)(H,60,70)(H,63,68)/t36-,46+,48+,50-,53+/m0/s1

SMILES

CC1CC(C2=C(N1C(=O)C)C=CC(=C2)C3=CC=C(C=C3)C(=O)NCCOCCOCCOCCOCC(=O)NC(C(=O)N4CC(CC4C(=O)NCC5=CC=C(C=C5)C6=C(N=CS6)C)O)C(C)(C)C)NC7=CC=C(C=C7)Cl

Mechanism

Target: MZP-55 targets BET proteins BRD2, BRD3, and BRD4, favoring BRD3/4 degradation.

Binding site: Its BRD3/4 ligand binds bromodomain acetyl-lysine recognition pockets.

Mechanism of action: MZP-55 is a VHL-recruiting BET PROTAC containing an I-BET726-based BET ligand connected to the VHL ligand VH032. This bifunctional design enables formation of BET–PROTAC–VHL ternary complexes, leading to ubiquitination and proteasome-dependent degradation of BET proteins. Reported data indicate strong depletion of BRD4 and BRD3, with weaker BRD2 degradation in certain cellular contexts. MZP-55 is useful for studying BET-family selectivity, chromatin-associated transcriptional regulation, c-MYC depletion, degrader potency, and comparative structure-activity relationships across VHL-based BET PROTAC scaffolds.

Applications

• PROTAC-Mediated Cancer Research: MZP-55 offers a novel approach for studying the degradation of oncogenic proteins in cancer research. By facilitating the selective degradation of target proteins, it aids in elucidating the roles these proteins play in tumorigenesis and provides insights into potential therapeutic strategies.

• Targeted Degradation in Neurodegenerative Diseases: Utilizing MZP-55 allows researchers to investigate the degradation of misfolded or aggregated proteins implicated in neurodegenerative disorders. This application facilitates a deeper understanding of protein homeostasis mechanisms and their potential exploitation for therapeutic intervention.

• PROTAC-Based Drug Discovery: MZP-55 serves as a valuable tool in the drug discovery process by enabling the targeted degradation of proteins previously considered "undruggable." This expands the landscape of potential drug targets and accelerates the development of innovative therapeutic agents.

• Mechanistic Studies of Protein Degradation: Researchers can employ MZP-55 to dissect the mechanistic pathways of proteasomal degradation. This application helps in understanding the intricacies of ubiquitin-proteasome system dynamics and the role of E3 ligases in targeted protein degradation.

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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂