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MK-5108

ATP-competitive inhibitor of AURKA

Structure

Information

  • AURKA
  • ATP-competitive inhibitor
  • 1 nM - 1 uM

In Vitro Validations

Uniprot ID: O14965
Target Class: Kinase
Target SubClass: cell cycle-regulated kinase
Potency: IC50
Potency Value: 0.064 nM
Potency Assay: Kinase Profiler Assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Aurora kinase A, STK6, STK15, IAK1, BTAK, AYK1, AU ...

DOI Reference: 10.1158/1535-7163.MCT-09-0609

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency end-point : IC50 AURKB 14.1 nM, AURKC 12.1 nM, TRKA 2 nM, TRKB 13 nM
Potency assay (off target): Kinase Profiler Assay
Probe Selectivity in Vitro:

MK-5108 was tested in the Kinase Profiler Assay against 233 kinases. MK-5108 does not bind to GABA receptors in vitro.

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SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This is an excellent probe to interrogate Aurora A kinase in vitro and in vivo. It has good selectivity over Aurora B (220-fold) and Aurora C (190-fold). It is known to inhibit only one kinase, TRKA, at less than 100-fold selectivity.

(last updated: 3 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This compound is reported to have good potency and selectivity for AurA, including over AurB and C. A wide range of cellular work has been published (see for example Chinn et al., J Cancer Res Clin Oncol, 2014, 140:1137–1149). Cellular potency ranges from ~0.2 to 1 uM. This appears to be an excellent and selective probe for AurA, and I am happy to recommend its use.

(last updated: 12 Sept 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 13 Mar 2017 )