612847-29-7Relevant academic research and scientific papers
Allosteric Akt (PKB) inhibitors: Discovery and SAR of isozyme selective inhibitors
Lindsley, Craig W.,Zhao, Zhijian,Leister, William H.,Robinson, Ronald G.,Barnett, Stanley F.,Defeo-Jones, Deborah,Jones, Raymond E.,Hartman, George D.,Huff, Joel R.,Huber, Hans E.,Duggan, Mark E.
, p. 761 - 764 (2005)
This letter describes the development of two series of potent and selective allosteric Akt kinase inhibitors that display an unprecedented level of selectivity for either Akt1, Akt2 or both Akt1/Akt2. An iterative analog library synthesis approach quickly provided a highly selective Akt1/Akt2 inhibitor that induces apoptosis in tumor cells and inhibits Akt phosphorylation in vivo.
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity
Zhao, Zhijian,Robinson, Ronald G.,Barnett, Stanley F.,Defeo-Jones, Deborah,Jones, Raymond E.,Hartman, George D.,Huber, Hans E.,Duggan, Mark E.,Lindsley, Craig W.
, p. 49 - 53 (2008/09/21)
This letter describes the development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved aqueous solubility (～18 mg/mL) that translates into enhanced cell activity and caspase-3 induction.
