KT109

KT109 : Inhibitor of DAGLB, ABHD6

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe KT109 is in the process of SERP review.

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Information

DAGLB
ABHD6

Inhibitor

100 nM

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: Q8NCG7

Target Class: Enzyme

Target SubClass: Lipase

Potency: IC50

Potency Value: 82 nM

Potency Assay: SAG substrate assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Diacylglycerol lipase-beta, DAGLB, DGLB_HUMAN, DGL ...

DOI Reference: 10.1038/nchembio.1105

Uniprot ID: Q8NCG7

Target Class: Enzyme

Target SubClass: Lipase

Potency: IC50

Potency Value: 42 nM

Potency Assay: Competitive ABPP assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Diacylglycerol lipase-beta, DAGLB, DGLB_HUMAN, DGL ...

DOI Reference: 10.1038/nchembio.1105

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): ABPP-SILAC analysis of serine hydrolase activities from Neuro2A cells treated in situ with KT109 (50 nM) for 4 h. KT109 inhibited DAGLβ and ABHD6 by ≥90% but did not inhibit any of the other detected serine hydrolases.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

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.

(last updated: 30 Apr 2023 )