SGC-GSK3-1 | SGC-GSK3-1 : Inhibitor of GSK3A and GSK3B
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
In Vivo
Control Compounds
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GSK3A
  • IC50:1.0 nM
  • IC50:4.6 nM
GSK3B
  • IC50:2.0 nM
  • IC50:12 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
SGC-GSK3-1 was analyzed at 1 μM in the Eurofins DiscoverX scanMAX panel (403 wild-type (WT) human as ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
200-fold selectivity window is observed between GSK3β and DYRK1B when comparing NanoBRET cellular ta ...

Potency
Cellular
In Vitro

GSK3A

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acschemneuro.3c00135

GSK3B

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acschemneuro.3c00135

Orthogonal Probes def

SGC-CDKL5/GSK3-1
SMILES: O=C(C1=NNC=C1NC(C2=CC(F)=CC(F)=C2)=O)NC3CCNCC3

Chemical Information

Molecular Formula C17H18F2N4O3
SMILEs O=C(NCC1CCOCC1)c1n[nH]cc1NC(=O)c1c(F)cccc1F
InChI InChI=1S/C17H18F2N4O3/c18-11-2-1-3-12(19)14(11)16(24)22-13-9-21-23-15(13)17(25)20-8-10-4-6-26-7-5-10/h1-3,9-10H,4-8H2,(H,20,25)(H,21,23)(H,22,24)
Molecular weight 364.13 Da
AlogP 0.0
HBond acceptors 7
HBond donors 3
Atoms 44

Expert Reviews


(on 17 Jun 2024 )
Cellular Use Rating
This is a good probe, with high in vitro and in-cell potency, a clear selectivity profile within the family, and proven target engagement. The compound is also safe for neuron cells. There is a related...
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