PLK4-IN-25

PLK4-IN-25 : Inhibitor of PLK4

Structure

SERP Rating

Probe PLK4-IN-25 is in the process of SERP review.

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Information

PLK4

Inhibitor

up to 500 nM

In Vitro Validations

Uniprot ID: O00444

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 7.9 ± 4.0 nM

Potency Assay: ADP-Glo assay

PDB ID for probe-target interaction (3D structure): 9Y9N

Target aliases:

Serine/threonine-protein kinase PLK4, STK18, SAK, ...

DOI Reference: 10.1021/acs.jmedchem.5c02200

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Eurofins KinaseProfile Selectivity Panel Data for Compound 25 at 1 µM

Probe Selectivity in Vitro:

A Eurofins KinaseProfiler selectivity panel containing 435 kinases was conducted to gain additional confidence in the experimental kinase selectivity assays. Fewer than 10% of the kinases screened were inhibited at greater than 50% at a single-point concentration of 1 μM.

Potency assay (off target): Biochemical assays with recombinant AURKB (ADP-Glo IC50 653 nM) and KDR (HTRF IC50 1600 nM ) confirmed selectivity against these targets.

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