1374264-52-4Relevant articles and documents
The discovery of SKLB-0335 as a paralog-selective EZH2 covalent inhibitor
Zhang, Qiangsheng,Hu, Xi,Li, Lu,Zhang, Lidan,Wan, Guoquan,Feng, Qiang,Zhu, Yongxia,Wang, Ningyu,Liu, Zhihao,Yu, Luoting
, p. 3006 - 3009 (2021/03/29)
By targeting the unique Cys663 of EZH2, SKLB-0335 displays high paralog-selectivity on EZH2. Biochemical studies show that SKLB-0335 can covalently bind to EZH2 at its S-adenosylmethionine (SAM) pocket and inhibit H3K27Me3. SKLB-0335 could be an effective chemical probe with which to further investigate the specific biological functions of EZH2.
ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
-
Page/Page column 94, (2013/12/03)
This invention relates to novel substituted benzamide according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.