MK-5108
MK-5108 : ATP competitive inhibitor of AURKA
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
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
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
(last updated: 13 Mar 2017 )