Tomivosertib

Inhibitor of MKNK1, MKNK2

Structure

SERP Rating

Probe Tomivosertib is in the process of SERP review.

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Information

MKNK1
MKNK2

Inhibitor

up to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: Q9BUB5

Target Class: Kinase

Target SubClass: CAMK

Potency: IC 50

Potency Value: 2.4 nM

Potency Assay: ADP-Glo kinase assay

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

Structure-activity relationship: yes

Target aliases:

MAP kinase-interacting serine/threonine-protein ki ...

DOI Reference: 10.1021/acs.jmedchem.7b01795

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : IC50 STK17A 130 nM, CLK4 790 nM

Probe Selectivity in Vitro:

Profiled for kinase selectivity at 1 uM over 400 kinases showing only 2 off-targets

Probe Selectivity in Cell:

Tomivosertib did not show antiproliferative activity in a panel of solid and hematological tumor cell lines (IC50 > 30 μM), modest sensitivity (IC50 < 10 μM) was observed in a subset of DLBCL and a multiple myeloma cell line.

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