MLi-2

Inhibitor of LRRK2

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe MLi-2 is in the process of SERP review.

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Information

Protein target names: LRRK2

Mechanism of action: Inhibitor

Primary References:

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

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

SERP 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

SERP 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 )