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KT109 | KT109 : Inhibitor of DAGLB, ABHD6
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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
DAGLB
  • IC50:82 nM
  • IC50:42 nM
  • IC50:14 nM
  • IC50:500 nM
  • INH:50 nM
ABHD6
  • IC50:16 nM
  • IC50:1 nM
Inhibitor
100 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
ABPP-SILAC analysis of serine hydrolase activities from Neuro2A cells treated in situ with KT109 (50 ...

Potency
Cellular
In Vitro

DAGLB

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/nchembio.1105

ABHD6

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/nchembio.1105

In Vivo Validations

Mouse
Dose: 0.1 - 10 mg/Kg
Route of delivery: Intraperitoneal

DOI Reference: 10.1038/nchembio.1105

Negative Control Compounds

KT195
Notes: KT195 showed negligible cross-reactivity with recombinant DAGLβ and concentration-dependent inhibition of ABHD6 as measured by competitive ABPP.

Chemical Information

Molecular Formula C27H26N4O
SMILEs O=C(N1CCCCC1Cc1ccccc1)n1cc(-c2ccc(-c3ccccc3)cc2)nn1
InChI InChI=1S/C27H26N4O/c32-27(30-18-8-7-13-25(30)19-21-9-3-1-4-10-21)31-20-26(28-29-31)24-16-14-23(15-17-24)22-11-5-2-6-12-22/h1-6,9-12,14-17,20,25H,7-8,13,18-19H2
Molecular weight 422.21 Da
AlogP 0.0
HBond acceptors 5
HBond donors --
Atoms 58

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 30 Apr 2023)
Cellular Use Rating
In Model Organisms
Best available in vitro probe for this target. However, the lack of pharmacokinetic data for the probe remains a limitation on its in vivo use. This should be considered before use in vivo.
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