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SGC6870 | SGC6870, an allosteric inhibitor of PRMT6
RATINGS:
Cellular Use: (2 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
PRMT6
  • IC50:77 nM
  • IC50:900 ± 100 nM
  • IC50:600 ± 100 nM
Allosteric
3 µM
up to 5 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: (R)-2 and (S)-2 were against a total of 33 methyltransferases, inc ...

Potency
Cellular
In Vitro

PRMT6

Mode of Action: Allosteric

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.0c02160

Negative Control Compounds

SGC6870N
Notes: SGC6870N Biochemical IC50 >50 uM, inactive in cells.
SMILES: CC1=CC([C@H]2C3=CC(C)=CC=C3NC(CN2C(C4=CC=C(S4)Br)=O)=O)=CC(C)=C1

Orthogonal Probes def

EPZ020411

Chemical Information

Molecular Formula C23H21BrN2O2S
SMILEs Cc1cc(C)cc([C@@H]2c3cc(C)ccc3NC(=O)CN2C(=O)c2ccc(Br)s2)c1
InChI InChI=1S/C23H21BrN2O2S/c1-13-4-5-18-17(11-13)22(16-9-14(2)8-15(3)10-16)26(12-21(27)25-18)23(28)19-6-7-20(24)29-19/h4-11,22H,12H2,1-3H3,(H,25,27)/t22-/m1/s1
Molecular weight 468.05 Da
AlogP 5.619760000000004
HBond acceptors 4
HBond donors 1
Atoms 50

Expert Reviews

by SERP
(on 16 Feb 2023)
Cellular Use Rating
(The reviewer did not leave any public comments)
by SERP+
(on 22 Mar 2023)
Cellular Use Rating
This probe has an excellent selectivity, no apparent off-targets or cytotoxicity, good negative control and orthogonal probes do exist. Although selectivity against off-targets for the panel of proteins...
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