ezh2 y641n

(S)-HH2853 is a potent dual inhibitor of EZH1 and EZH2, inhibiting EZH2_Y641F with an IC50 of <100 nM.(S)-HH2853 has potential antitumor activity and can be used in the study of autoimmune diseases.

HDACs EZH2-IN-1 (Compound 22a) is a dual inhibitor of HDACs and EZH2, exhibiting potent inhibitory activity, with EZH2 Y641N being suppressed by 98% at 50 nM. It selectively targets HDAC1 and HDAC6, with IC50 values of 0.23 μM and 0.07 μM, respectively. HDACs EZH2-IN-1 effectively inhibits the proliferation of diffuse large B-cell lymphoma cells harboring EZH2 mutations and various acute myeloid leukemia cells. Additionally, this compound has the capability to induce cellular differentiation and apoptosis (Apoptosis).

EZH2-IN-8 is a potent inhibitor of EZH2 with potential applications in cancer disease research.

CPI-169 racemate (CPI 169) is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.

PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 (Kis: 0.7 and 3.0 nM, respectively).

EZH2-IN-19 (compound N40) is a potent inhibitor of the wild-type enhancer of zeste homolog 2 (EZH2), with an IC50 of 0.32 nM. It plays a significant role in cancer research.

EZH2-IN-9 is a potent inhibitor of EZH2, which, through overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations), causes abnormal elevations in H3K27me3 and contributes to the growth and development of various tumours (e.g., breast cancer, prostate cancer, leukaemia). EZH2-IN-9 has shown potential for cancer research.

IHMT-EZH2-426 (compound 38) is a potent covalent degrader of EZH2, demonstrating IC50 values of 1.3 nM for EZH2 wild-type, 1.2 nM for EZH2-A687V, and 1.7-3.5 nM for EZH2-Y641F Y641N Y641S mutants. The compound effectively inhibits proliferation in B-cell lymphoma and triple-negative breast cancer (TNBC) cell lines due to its capacity to diminish H3K27me3 and EZH2 levels [1].

EZH2-IN-22 (example 92) is a potent EZH2 inhibitor, exhibiting IC50 values of <0.00051 µM for EZH2(Y641N) and EZH2(Y641F), and 0.00052 µM for EZH2 (wt). Additionally, EZH2-IN-22 demonstrates antiproliferative activity.

PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.

EZH2-IN-7, a potent inhibitor of EZH2, addresses overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) that cause an abnormal increase in H3K27me3, contributing to the proliferation of various tumors, including breast cancer, prostate cancer, and leukemia. It shows promise for cancer research applications.