Mz1, selectively degrades BRD4 (ab230371)

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Overview

  • Product name

    Mz1, selectively degrades BRD4

  • Description

    (+)-JQ1 based PROTAC that selectively degrades BRD4

  • Biological description

    Cell penetrant PROTAC (Proteolysis Targeting Chimera) compound based on (+)-JQ1 (ab141498) tethered to a von Hippel-Lindau (VHL) ligand. Retains high affinity for BRD2, BRD3 and BRD4 bromodomains. Induces preferential degradation of BRD4 over BRD2 and BRD3 in HeLa cells.

  • Purity

    > 98%

  • CAS Number

    1797406-69-9

  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    (2S,4R)-1-((S)-2-(tert-Butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2- f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)- 4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

  • Molecular weight

    1002.64

  • Molecular formula

    C49H60ClN9O8S2

  • PubChem identifier

    122201421

  • Storage instructions

    Shipped at 4°C. Store at -20°C.

  • SMILES

    CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCOCCOCCOCC(=O)NC(C(=O)N4CC(CC4C(=O)NCC5=CC=C(C=C5)C6=C(N=CS6)C)O)C(C)(C)C)C7=CC=C(C=C7)Cl)C

  • Source

    Synthetic

References

This product has been referenced in:

  • Gadd MS  et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol 13:514-521 (2017). Read more (PubMed: 28288108) »
  • Zengerle M  et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chem Biol 10:1770-7 (2015). Read more (PubMed: 26035625) »

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