A-800141 is an orally active and selective MetAP2 inhibitor with an IC50 of 12 nM. A-800141 has weak inhibitory activity for MetAP1 (IC50 : 36 μM). GAPDH can be used as a biomarker to monitor the MetAP2 inhibition of A-800141. A-800141 has antiangiogenic and anticancer activity in a variety of xenograft tumor models[1].
References
[1] Wang J, et al. Correlation of tumor growth suppression and methionine aminopetidase-2 activity blockade using an orally active inhibitor. Proc Natl Acad Sci U S A. 2008 Feb 12;105(6):1838-43. DOI:10.1073/pnas.0708766105
