TP-020

Inhibitor of MGAT2

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe TP-020 is in the process of SERP review.

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Information

MGAT2

Inhibitor

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Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: Q10469

Target Class: Other post-translational modification

Target SubClass: N-acetylglucosaminyltransferase

Potency: IC50

Potency Value: 7.8 nM (human) 2.4 nM (Mouse)

Potency Assay: Enzymatic Assay

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

Target aliases:

Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglu ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : IC50 MGAT1 2.6 uM, DGAT1 >30 uM, DGAT2 >30 uM , ACAT1 19 uM

Probe Selectivity in Cell:

KinomeSCAN and GPCR scan available from SGC

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Probe molecule was evaluated against MGAT2 in vitro, but not in cells. Evaluated against recombinant preparations of DGAT1, DGAT2 and ACAT1 shows selectivity for MGAT2. No data shown for other MGAT isoforms. Not enough off-target or in cell validation performed to fully evaluate selectivity in original publication. Probe shown to inhibit triglyceride production at various concentrations (1–30 mg/kg) in mice. Use with appropriate controls.

(last updated: 24 Sept 2020 )