IHMT-EZH2-426

IHMT-EZH2-426 (compound 38) potently inhibits EZH2 WT and various EZH2^Y641 mutants, with IC₅₀ values ranging from 1.3 nM to 11 nM; in the AlphaLISA enzyme inhibition assay, it shows 113-fold higher selectivity for EZH2 WT than for EZH1 WT^[1].
IHMT-EZH2-426 (0.03-10 μM; 72 h) inhibits H3K27 trimethylation at a concentration of 0.03 μM and reduces EZH2 protein levels at 1 μM after 72 h of treatment in Karpas-422, Pfeiffer, MDA-MB-231 and MDA-MB-468 cell lines^[1].
IHMT-EZH2-426 (10 μg/mL; 72 h treatment, up to 48 h washout) achieves sustained inhibition of H3K27me3 for at least 48 h after washout in MDA-MB-231 cells, confirming its persistent binding to the target^[1].
IHMT-EZH2-426 (1-50 μM; 4 h compound treatment, 4 h probe incubation) binds to EZH2 in MDA-MB-231 cell lysates, and labels approximately 50% of available target proteins at a concentration of 1 μM^[1].
IHMT-EZH2-426 forms a covalent adduct with purified EZH2 (SET domain) protein, confirming its covalent binding mechanism^[1].
IHMT-EZH2-426 (0.1-10 μM; 5 days) potently inhibits the proliferation of EZH2-mutant B-cell lymphoma cell lines (GI₅₀ 0.02-3.85 μM), and exhibits moderate antiproliferative activity against EZH2-wild-type B-cell lymphoma cell lines as well as triple-negative breast cancer (TNBC) cells (GI₅₀ 1.93-7.01 μM)^[1].
IHMT-EZH2-426 (for 14 days) inhibits colony formation of MDA-MB-231 and MDA-MB-468 triple-negative breast cancer (TNBC) cells in a dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.