Uses
CPI-169 is a heteroaryl amide that was discovered useful as modulator of Me modifying enzymes.
Definition
ChEBI: 1-[1-(1-ethylsulfonyl-4-piperidinyl)ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-indolecarboxamide is an indolecarboxamide.
Biological Activity
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].
References
[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
