JJKK-048

JJKK-048 : Inhibitor of MGLL

Structure

SERP Rating

Probe JJKK-048 is in the process of SERP review.

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Information

MGLL

Inhibitor

10 nM

Probe Availability:

In Vitro Validations

Uniprot ID: Q99685

Target Class: Enzyme

Target SubClass: Lipase

Potency: IC50

Potency Value: 0.363 nM

Potency Assay: In competitive ABPP, JJKK-048 prevented TAMRA-fluorophosphonate (FP) labeling of the MAGL active site serine (S122).

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

Target aliases:

Monoglyceride lipase, MGLL, MGLL_HUMAN, MAGL, MGL, ...

DOI Reference: 10.1016/j.chembiol.2013.01.012

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Activity assays using rat and human FAAH preparations revealed that JJKK-048 exhibited notable MAGL selectivity over FAAH (JJKK-048 > 13,000-fold). Activity assays with human ABHD6 indicated that JJKK-048, the MAGL/ABHD6 selectivity ratio was ∼630-fold. Human ABHD12 was resistant to JJKK-048 (remaining activity, 91.7% ± 0.3% at 10−6 M). Competitive ABPP of serine hydrolases in mouse brain membrane proteome using TAMRA-FP indicated that MAGL was the only detectable target of JJKK-048 at concentrations up to 10−7 M. No binding to CB1R or CB2R.

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