Novel Science

TK216 (ets-Family Transcription Factor Inhibitor)


Blocking the road, stopping the engine or killing the driver? Advances in targeting EWS/FLI-1 fusion in Ewing sarcoma as novel therapy. Kovar, H. (2014) Expert Opinion Therapeutic Targets [Early Online]

A Small Molecule Inhibitor of ETV1, YK-4-279, Prevents Prostate Cancer Growth and Metastasis in a Mouse Xenograft Model. Rahim, S., et al. (2014) PLoS ONE 9(12); 1-20

Pharmacokinetic modeling optimizes inhibition of the ‘undruggable’ EWS-FLI1 transcription factor in Ewing Sarcoma. Hong, S-Y., et al. (2013) Oncotarget 5(2); 338-350

Single Enantiomer of YK-4-279 Demonstrates Specificity in Targeting the Oncogene EWS-FLI1. Barber-Rotenberg, J., et al. (2012) Oncotarget 4(2); 172-182

A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing’s sarcoma. Erkizan, H., et al. (2009) Nature Medicine 15(7); 750-757


TK216, a Novel, Small Molecule Inhibitor of the ETS-Family of Transcription Factors, Displays Anti-Tumor Activity in AML and DLBCL. Jessen, K. et al.American Society of Hematology Annual Meeting Poster, December 2016. Available upon request.