tcs-pim-1-4a-smi-4a

Description: TCS-PIM-1-4a ( (the mixture of E- and Z-enantiomers of SMI-4a) is a novel Pim inhibitor with IC50 of 13 nM for Pim-1 and 2.3 uM for Pim-2. The Pim protein kinases are frequently overexpressed in prostate cancer and certain forms of leukemia and lymphoma. TCS-PIM-1-4a was identified by screening to be a Pim-1 inhibitor and was found to attenuate the autophosphorylation of tagged Pim-1 in intact cells. Although TCS-PIM-1-4a is a competitive inhibitor with respect to ATP, a screen of approximately 50 diverse protein kinases demonstrated that it has high selectivity for Pim kinases. Overall, TCS-PIM-1-4a represents a new Pim kinase inhibitor that may provide leads to novel anticancer agents.

References: Proc Natl Acad Sci U S A. 2011 Jan 11; 108(2):528-33.; Mol Cancer Ther. 2009 Jun; 8(6):1473-83; Blood. 2010 Jan 28; 115(4):824-33.