The discovery of SKLB-0335 as a paralog-selective EZH2 covalent inhibitor?
Chemical Communications Pub Date: 2021-02-02 DOI: 10.1039/D0CC04670A
Abstract
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.
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Journal Name：Chemical Communications
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CAS no.: 89640-58-4
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