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MZP-54 - CAS 2010159-47-2

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MZP-54 is a PROTAC targeting on BET, consist of a warhead I-BET726 (BET bromodomain inhibitor) linked to a VHL ligand VH032. It exhibited affinity to the Brd4BD2 and VHL-EloC-EloB protein with Kd values of 4nM and 105nM, respectively. Treatment with 50nM MZP-54 for 4h led to degradation of Brd4 by 87%, accompanied with the downregulation of c-MYC by 73% in MV4;11 cells.

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Molecular Formula
C55H66ClN7O9S
Molecular Weight
1036.67

MZP-54

    • Specification
      • Solubility
        Ethanol : 50 mg/mL (48.23 mM; Need ultrasonic)
        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-54; MZP 54; MZP54; (2S,4R)-1-[(2S)-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]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
    • Properties
      • InChI Key
        FYSWLIFIYIVHPI-DDWISSAJSA-N
        InChI
        InChI=1S/C55H66ClN7O9S/c1-34-27-46(60-43-18-16-42(56)17-19-43)45-28-41(15-20-47(45)63(34)36(3)64)38-11-13-40(14-12-38)52(67)57-21-22-70-23-24-71-25-26-72-32-49(66)61-51(55(4,5)6)54(69)62-31-44(65)29-48(62)53(68)58-30-37-7-9-39(10-8-37)50-35(2)59-33-73-50/h7-20,28,33-34,44,46,48,51,60,65H,21-27,29-32H2,1-6H3,(H,57,67)(H,58,68)(H,61,66)/t34-,44+,46+,48-,51+/m0/s1
        Canonical SMILES
        CC1CC(C2=C(N1C(=O)C)C=CC(=C2)C3=CC=C(C=C3)C(=O)NCCOCCOCCOCC(=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
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