PPM-3

PPM-3 : Degrader (PROTAC) of MAPK7

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe PPM-3 is in the process of SERP review.

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Information

MAPK7

Degrader (PROTAC)

up to 500 nM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q13164

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 62.4 ± 18.6 nM

Potency Assay: ADP-Glo Assay

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

Target aliases:

Mitogen-activated protein kinase 7, PRKM7, ERK5, B ...

DOI Reference: 10.1021/acs.jmedchem.3c00864

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): PPM-3 demonstrated outstanding kinase selectivity among more than 300 kinases at 500 nM in terms of kinase inhibition.

Potency assay, off target (cells): The ligand component of PPM-3 may also target bromodomain-containing protein 4 (BRD4), doublecortin-like kinase 1 (DCLK1), and leucine-rich repeat kinase 2 (LRRK2). The proteins produced by A375 cells treated with PPM-3 at various concentrations for 12 h were assessed via Western blotting. PPM-3 degraded ERK5, but not BRD4, LRRK2 or DCLK1.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Degradation of ERK5 by PPM-3 begins within 2-4 hours and peaks at 12 hours. Proteomics analysis was performed at a late time point (48 h) which therefore may include secondary effects. The selectivity profile is relatively good considering that the biological assay has been performed with 0.5 uM compound which could skew the results of the selectivity profile presented in the paper.

(last updated: 20 Feb 2025 )