IHMT-EZH2-426 is a potent covalent degrader of EZH2, demonstrating IC50 values of 1.3 nM for wild-type EZH2 and 1.2 nM and 1.7-3.5 nM against the mutants EZH2-A687V and EZH2-Y641F/Y641N/Y641S, respectively. This compound effectively reduces levels of H3K27me3 and EZH2, exhibiting significant anti-proliferative activity in B-cell lymphoma and triple-negative breast cancer (TNBC) cell lines. It is a valuable tool for research aimed at understanding EZH2's role in oncogenesis and potential therapeutic interventions.
IHMT-EZH2-426 is a potent covalent degrader of EZH2, demonstrating IC50 values of 1.3 nM for wild-type EZH2 and 1.2 nM and 1.7-3.5 nM against the mutants EZH2-A687V and EZH2-Y641F/Y641N/Y641S, respectively. This compound effectively reduces levels of H3K27me3 and EZH2, exhibiting significant anti-proliferative activity in B-cell lymphoma and triple-negative breast cancer (TNBC) cell lines. It is a valuable tool for research aimed at understanding EZH2's role in oncogenesis and potential therapeutic interventions.
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