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MS8709 | MS8709 : Degrader (PROTAC) of EHMT2, EHMT1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
EHMT2
    • Dmax:>99%
    • DC50:274 ± 2 nM
    EHMT1
      • Dmax:>99%
      • DC50:260 ± 53 nM
      Degrader (PROTAC)
      3 uM

      Selectivity

      In Vitro Selectivity Assessment
      Potency Assay Off-Target:
      Selectivity of MS8907 (at 10 μM) against a panel of 21 protein methyltransferases was assessed using ...

      Potency
      Cellular
      In Vitro

      EHMT2

      Mode of Action: Degrader (PROTAC)

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1021/acs.jmedchem.3c02394

      EHMT1

      Mode of Action: Degrader (PROTAC)

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1021/acs.jmedchem.3c02394

      In Vivo Validations

      Mouse
      Dose: 50 mg/Kg
      Route of delivery: Intraperitoneal
      Plasma half life: 1.5 h
      Cmax: 27 ± 0.6 μM
      Tmax: 0.5 h
      Area Under the Curve:: 61 ± 3 h*uM

      DOI Reference: 10.1021/acs.jmedchem.3c02394

      Negative Control Compounds

      canSAR7412571
      Notes: cpd 14 is able to inhibit G9A and GLP but not to degrade them.

      Chemical Information

      Molecular Formula C64H95F2N11O7S
      SMILEs COc1cc2c(NC3CCN(CCCC(=O)NCCCCCCCCCCCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)nc(N3CCC(F)(F)CC3)nc2cc1OCCCN1CCCC1
      InChI InChI=1S/C64H95F2N11O7S/c1-45-57(85-44-69-45)47-23-21-46(22-24-47)42-68-60(81)52-39-49(78)43-77(52)61(82)58(63(2,3)4)72-56(80)19-13-11-9-7-6-8-10-12-14-29-67-55(79)20-17-32-75-34-25-48(26-35-75)70-59-50-40-53(83-5)54(84-38-18-33-74-30-15-16-31-74)41-51(50)71-62(73-59)76-36-27-64(65,66)28-37-76/h21-24,40-41,44,48-49,52,58,78H,6-20,25-39,42-43H2,1-5H3,(H,67,79)(H,68,81)(H,72,80)(H,70,71,73)/t49-,52+,58-/m1/s1
      Molecular weight 1199.71 Da
      AlogP 9.65332
      HBond acceptors 18
      HBond donors 5
      Atoms 180

      Vendors

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      Expert Reviews

      by SERP
      (on 13 Jun 2024 )
      Cellular Use Rating
      In Model Organisms
      MS8709 was well tolerated at a single IP dose of 50 mg/kg. It is recommended a MTD study is carried out before any repeat dosing efficacy model studies.
      by SERP+
      (on 6 Feb 2026 )
      Cellular Use Rating
      In Model Organisms
      The probe's selectivity was characterised within the family, but proteome-wide selectivity assessment (global proteomics) is missing. Against three of the 21 tested protein methyltansferases (EZH2, PRMT7,...
      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