Chemical Probes logo
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
Download

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

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

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