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EZM0414 is an inhibitor of SET domain-containing protein 2 (SETD2, IC50 = 18 nM). It inhibits the proliferation of A549 non-small cell lung cancer (NSCLC) cells (EC50 = 57 nM). EZM0414 (15 and 30 mg/kg) decreases tumor volume in a KMS-11 multiple myeloma mouse xenograft model. It decreases cardiomyocyte levels of trimethylated lysine 36 on histone H3 (H3K36Me3) in a mouse model of heart failure with preserved ejection fraction (HFpEF) induced by a high-fat diet and L-NAME (Cay-80210). EZM0414 also reduces lung congestion and cardiac hypertrophy in the same model. InChI: InChI=1S/C22H29FN4O2/c1-14-6-7-19(23)18-13-20(25-21(14)18)22(29)24-16-4-3-5-17(12-16)27-10-8-26(9-11-27)15(2)28/h6-7,13,16-17,25H,3-5,8-12H2,1-2H3,(H,24,29)/t16-,17+/m1/s1, InChIKey: PGNLXEBQMQHFNK-SJORKVTESA-N, SMILES: FC1=C2C(NC(C(N[C@@H]3CCC[C@@H](C3)N4CCN(CC4)C(C)=O)=O)=C2)=C(C=C1)C
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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