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SGC-GAK-1 | SGC-GAK-1 : Inhibitor of GAK
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 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
GAK
  • Kd:1.9 nM
  • IC50:110 nM
  • IC50:650 nM
  • IC50:170 nM
Inhibitor
up to 1 µM; use with appropriate control compounds

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
No kinases were observed to bind SGC-GAK-1 within 30-fold of the KD of GAK in a KINOMEscan assay (Di ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Despite weakly binding RIPK2 in vitro (DiscoverX RIPK2 KD = 110 nM; 58-fold of GAK KD), SGC-GAK-1 po ...

Potency
Cellular
In Vitro

GAK

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.8b01213

Negative Control Compounds

SGC-GAK-1N
SMILES: CN(C1=CC(OC)=C(OC)C(OC)=C1)C2=C3C(C=CC(C(F)(F)F)=C3)=NC=C2
KA2
Notes: HY-19764, highly cell-potent RIPK2 ligand (IC50 = 2.2 nM), lacks GAK affinity (IC50 > 10 µM).

Chemical Information

Molecular Formula C18H17BrN2O3
SMILEs COc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
InChI InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
Molecular weight 388.04 Da
AlogP 4.766700000000004
HBond acceptors 5
HBond donors 1
Atoms 41

Vendors

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Expert Reviews

by SERP
(on 21 Jun 2022)
Cellular Use Rating
This set of probes, including SGC-GAK-1 and SGC-GAK-1N and KA2 together represent the current best available chemical tools for deciphering GAK function in cells. KINOMEscan and cellular nanobret target...
by SERP
(on 6 Jul 2022)
Cellular Use Rating
Partial engagement of RIPK2 was reported at 1µM, effects at higher concentrations should be interpreted accordingly
by SERP+
(on 22 Mar 2023)
Cellular Use Rating
Cellular engagement with RIPK2 was reported at 0.4µM, hence the probe should be used in combination with selective RIPK2 inhibitors (e.g., HY-19764) as an orthogonal tool.
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