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SGC3027 | SGC3027 : Prodrug, SAM-competitive of PRMT7
RATINGS:
Cellular Use: (1 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
PRMT7
  • IC50:<2.4 nM
  • Kd:6.4 ± 1.2 nM
  • IC50:294 ± 26 nM
  • IC50:2400 ± 100 nM
Prodrug, SAM-competitive
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Good selectivity over a panel of 35 methyltransferases including PRMTs and kinases. RIPK2: 81% inhib ...

Potency
Cellular
In Vitro

PRMT7

Mode of Action: Prodrug, SAM-competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41467-020-16271-z

Negative Control Compounds

CANSAR3883275
Notes: SGC3027N (SGC8158N IC50 14 ± 2 µM against PRMT7) cellular IC50 higher than 100 µM

Chemical Information

Molecular Formula C41H47ClN6O6S
SMILEs CC1=C(C)C(=O)C(C(C)(C)CC(=O)N(CCCCSC[C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)Cc2cccc(-c3ccc(Cl)cc3)c2)=C(C)C1=O
InChI InChI=1S/C41H47ClN6O6S/c1-23-24(2)35(51)32(25(3)34(23)50)41(4,5)18-31(49)47(19-26-9-8-10-28(17-26)27-11-13-29(42)14-12-27)15-6-7-16-55-20-30-36(52)37(53)40(54-30)48-22-46-33-38(43)44-21-45-39(33)48/h8-14,17,21-22,30,36-37,40,52-53H,6-7,15-16,18-20H2,1-5H3,(H2,43,44,45)/t30-,36-,37-,40-/m1/s1
Molecular weight 786.30 Da
AlogP 0.0
HBond acceptors 12
HBond donors 4
Atoms 102
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

Expert Reviews

by SERP
(on 22 May 2023 )
Cellular Use Rating
SGC3027 is recommended as a selective inhibitor of PRMT7 for in vitro experiments including studies in cells. No information is known about the PK of SGC3027 so it is not recommended for in vivo studies. Note...
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