UNC6852 | UNC6852 : Degrader (PROTAC) of EED and PRC complex
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
In Vivo

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
EED
  • IC50:247 nM
  • EC50:790 nM
  • DC50:610 nM
  • EC50:3400 nM
  • Dmax:92%
  • Dmax:94%
  • Activity:10 µM
EZH2
    • DC50:300 nM
    • DC50:670 nM
    • Dmax:64%
    • Dmax:96%
    SUZ12
      • DC50:590 nM
      • Dmax:22%
      • Dmax:82%
      Degrader (PROTAC)
      10 µM to reliably degrade the target
      up to 10 uM

      Selectivity

      In Vitro Selectivity Assessment
      Potency Assay Off-Target:
      Global proteomics experiments using tandem mass tag quantification comparing HeLa cells treated with ...
      Selectivity Assessment Description:
      EED and EZH2 were selectively degraded by UNC6852 within the proteome. Modest SUZ12 degradation (21% ...

      Potency
      Cellular
      In Vitro

      EED

      Mode of Action: Degrader (PROTAC)

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1016/j.chembiol.2019.11.006

      EZH2

      Mode of Action: Degrader (PROTAC)

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1016/j.chembiol.2019.11.006

      SUZ12

      Mode of Action: Degrader (PROTAC)

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1016/j.chembiol.2019.11.006

      Negative Control Compounds

      UNC7043
      SMILES: Cc1c(c2ccc(CNC([C@@H]3C[C@@H](CN3C([C@H](C(C)(C)C)NC(CCCNC(c4ccc(c(cnc5NCc6occc6)c7n5cnn7)cc4)=O)=O)=O)O)=O)cc2)scn1

      Chemical Information

      Molecular Formula C43H48N10O6S
      SMILEs Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCNC(=O)c2ccc(-c3cnc(NCc4ccco4)n4cnnc34)cc2)C(C)(C)C)cc1
      InChI InChI=1S/C43H48N10O6S/c1-26-36(60-25-48-26)29-11-9-27(10-12-29)20-45-40(57)34-19-31(54)23-52(34)41(58)37(43(2,3)4)50-35(55)8-5-17-44-39(56)30-15-13-28(14-16-30)33-22-47-42(53-24-49-51-38(33)53)46-21-32-7-6-18-59-32/h6-7,9-16,18,22,24-25,31,34,37,54H,5,8,17,19-21,23H2,1-4H3,(H,44,56)(H,45,57)(H,46,47)(H,50,55)/t31-,34+,37-/m1/s1
      Molecular weight 832.35 Da
      AlogP 0.0
      HBond acceptors 16
      HBond donors 5
      Atoms 108

      Vendors

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      Expert Reviews


      (on 16 Mar 2022)
      Cellular Use Rating
      Degradation of target proteins is dependent on cellular VHL expression. The activity may be lower / recommended cellular concentration higher in cells with low VHL expression (e.g., platelets). Degradation...
      (on 10 Apr 2022)
      Cellular Use Rating
      (The reviewer did not leave any public comments)
      (on 6 Feb 2026)
      Cellular Use Rating
      UNC6852 is an EED-targeted, VHL-recruiting bivalent chemical degrader. Degradation of EED leads to co-degradation of the other core PRC2 subunit EZH2, with more modest degradation of SUZ12. UNC6852 was...
      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