MK-5108

Reagent Authentication Certificate:

Chemical Probes Portal MK-5108.pdf

Protein target name:

AURKA

Mechanism of action:

ATP-competitive inhibitor

Recommended Concentration for use in cells:

1 nM - 1 uM

Probe Availability

Cayman (1010085-13-8)

MedChem Express (1010085-13-8)

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

cell cycle-regulated kinase

HUGO ID:

HGNC:11393

Entrez gene ID:

6790

UNIPROT ID:

O14965

Target alias:

AIK, ARK1, AURA, BTAK, PPP1R47, STK15, STK6, STK7

Probe Details

Chemical Probes Portal ID:

CPP134

Probe alias:

1010085-13-8, VX-689, MK5108, MK 5108, MK-5108

PubChem CID:

24748204

ChEMBL ID:

CHEMBL3600873

SMILES string:

FC(C(Cl)=CC=C1)=C1O[C@H](CC2)CC[C@@]2(C(O)=O)CC3=CC=CC(NC4=NC=CS4)=N3

InChi Key:

LCVIRAZGMYMNNT-UHFFFAOYSA-N

Orthogonal probe:

AMG900XMD-12

PAINs evaluation:

PAINs free

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

0.064 nM

Potency assay:

Kinase Profiler Assay

Off target activity

Potency (off target):

IC50

Off target protein and potency:

AURKB 14.1 nMAURKC 12.1 nMTRKA 2 nMTRKB 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.

In cell validation

On target activity in cells

Potency assay (cells):

In cells, MK-5108 inhibited AURKA autophosphorylation and the accumulation of phosphoH3 in response to DNA damage.

Target engagement assay (cells):

Indirect: inhibition of autophosphorylation

Primary Reference

Reference (doi):

10.1158/1535-7163.MCT-09-0609

Reference (PMID):

20053775

Endorsed probe

The Chemical Probes Portal endorses this compound as chemical probe for use in cells and in model organisms.

SAB Rating

Rating for use in Cells

3 review(s)

Rating for use in Model Organisms

3 review(s)

SAB Members

SAB 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.

Jun 12 2016 - 2:22pm

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.

Sep 12 2016 - 6:31pm

MK-5108

Probe Availability

Probe Information

Target Details

AIK, ARK1, AURA, BTAK, PPP1R47, STK15, STK6, STK7

Probe Details

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

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MK-5108

Probe Availability

Probe Information

Target Details

AIK, ARK1, AURA, BTAK, PPP1R47, STK15, STK6, STK7

Probe Details

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?