EZH2-IN-17 (compound 28) is a potent and orally active EZH2 inhibitor with an IC50 value of 0.95 nM. EZH2-IN-17 exhibits high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively)[1].
References
[1] Xin Xu, et al. Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2). Bioorg Med Chem Lett. 2023 Nov 11:129558. DOI:10.1016/j.bmcl.2023.129558
