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MZP-54 | MZP-54 : Degrader (PROTAC) of BRD2, BRD3, BRD4
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
BRD2
    • Dmax:42 %
    BRD3
      • DC 50:50 nM
      • EC 50:49 nM
      • Dmax:91%
      BRD4
      • Kd:4±2 nM
      • DC 50:8-25 nM
      • Dmax:98-85%
      • EC 50:269 nM
      Degrader (PROTAC)
      100 nM

      Selectivity

      Potency
      Cellular
      In Vitro

      BRD2

      Mode of Action: Degrader (PROTAC)

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1021/acs.jmedchem.6b01912

      BRD3

      Mode of Action: Degrader (PROTAC)

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1021/acs.jmedchem.6b01912

      BRD4

      Mode of Action: Degrader (PROTAC)

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1021/acs.jmedchem.6b01912

      Orthogonal Probes def

      I-BET151

      Chemical Information

      Molecular Formula C55H66ClN7O9S
      SMILEs CC(=O)N1c2ccc(-c3ccc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)cc3)cc2[C@H](Nc2ccc(Cl)cc2)C[C@@H]1C
      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
      Molecular weight 1035.43 Da
      AlogP 7.3259200000000115
      HBond acceptors 16
      HBond donors 5
      Atoms 139

      References

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      Expert Reviews

      by SERP
      (on 21 Feb 2021 )
      Cellular Use Rating
      This compound has the unique properties of selectively degrading BRD3 and BRD4 at low nanomolar concentration, while not affecting BRD2. It thereby shows a distinct profile from other BET bromodomain...
      by SERP
      (on 26 Mar 2021 )
      Cellular Use Rating
      While there are better degraders for BRD4, it offers an orthogonal probe to the JQ1 derived degraders that the authors had previously disclosed. It also demonstrates slightly different selectively...
      by SERP
      (on 20 Feb 2025 )
      Cellular Use Rating
      This compound degrades BRD3 as well as BRD4. Unfortunately, no proteomics data have been provided. It is a useful compound as an orthogonal chemical probe, in particular as it does have an orthogonal warhead...
      Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria