Background:

CPI-169 is a novel, small molecule and potent inhibitor of enhancer of zeste homolog 2 (EZH2) with an IC50 value of<1nM for polycomb repressive complex 2 (PRC2) [1].

CPI-169 has been found to be a potent EZH2 inhibitor with an IC50 value of<1nM for polycomb repressive complex 2 (PRC2). In addition, CPI-169 has been reported to reduce cellular levels of histone H3 on lysine 27(H3K27) with an EC50 value of 70nM. Moreover, CPI-169 has been exhibited to trigger cell cycle arrest and apoptosis in cells. Apart from these, treatment the inhibitor at 200mpk twice daily, CPI-169 has been noted to have a well tolerated in mice with no observed toxic effect or body weight loss [1].

参考文献:
[1] Vidya Balasubramanian, Priya Iyer, Shilpi Arora, Patrick Troyer, Emmanuel Normant. Constellation Pharmaceuticals, Cambridge, MA. CPI-169, a novel and potent EZH2 inhibitor, synergizes with CHOP in vivo and achieves complete regression in lymphoma xenograft models