MLi-2

Inhibitor of LRRK2

Structure

Information

Protein target names: LRRK2

Mechanism of action: Inhibitor

In Vitro Validations

Uniprot ID: Q5S007
Target Class: Protein kinase
Target SubClass: TKL
Potency: IC50
Potency Value: 1.8 nM
Potency Assay: MSD and Invitrogen assay
PDB ID for probe-target interaction (3D structure): 5U6I
Structure-activity relationship: yes see ref. DOI: 10.1021/acs.jmedchem.7b00045
Target aliases:
Leucine-rich repeat serine/threonine-protein kinas ...

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

Comments:

In a mouse model of idiopathic PD, MLi-2 was well-tolerated and showed robust target engagement. However, LRRK2 kinase inhibition in the MitoPark model did not prevent motor dysfunction, α-synuclein pathology or neuron death.

(last updated: 5 Jun 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

While there are multiple commercially available LRRK inhibitors available, MLi-2 provides another quality chemical probe to help validate this target in cell-based assays.

(last updated: 3 Jul 2020 )