GSK126, EZH2 methyltransferase inhibitor

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(2 Publications)

MW 526.7 Da. Potent inhibitor EZH2 methyltransferase inhibitor (K_i = 93 pM). Selective (>150-fold) versus EZH1. Greater than 1000-fold selective against a panel of 20 other human methyltransferases including both SET-domain-containing and non-SET-domain-containing methyltransferases. Decreases global H3K27me3 levels. Inhibits B-cell lymphoma cell proliferation in vitro. Inhibits EZH2 mutant tumor growth in xenograft models. Reactivates silenced PRC2 target genes and inhibits the proliferation of EZH2 mutant DLBCL cell lines and corresponding xenografts mice. Literature suggests that GSK126 is a potential treatment for EZH2 mutant lymphoma (McCabe et al).

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AD 003, Alpha N-terminal protein methyltransferase 1A, C9orf32, CHET9, ChET 9 protein, Chromatin precipitated E2F target 9 protein, Chromosome 9 open reading frame 32, EED protein, EED, mouse, homolog of, EED_HUMAN, ENX-1, EZH2_HUMAN, EZH2b, Embryonic ECTODERM development protein homolog, Embryonic ectoderm development, Embryonic ectoderm development isoform a, Embryonic ectoderm development protein, mouse, homolog of, Enhancer of zeste 2, Enhancer of zeste homolog 2, Enhancer of zeste homolog 2 (Drosophila), Enhancer of zeste, Drosophila, homolog 2, Enx 1h, Histone-lysine N-methyltransferase EZH2, JJAZ1, Joined to JAZF1 protein, KIAA0160, KMT 6, KMT6A, Lysine N-methyltransferase 6, MGC9169, Methyltransferase like 11A, Methyltransferase-like protein 11A, N-terminal RCC1 methyltransferase, NRMT, NTM1A_HUMAN, NTMT1, OTTHUMP00000235483, OTTHUMP00000235484, OTTHUMP00000235485, Polycomb protein SUZ12, Polycomb protein eed, SUZ12 polycomb repressive complex 2 subunit, SUZ12_HUMAN, Suppressor of zeste 12 homolog, Suppressor of zeste 12 protein homolog, WAIT-1, WD protein associating with integrin cytoplasmic tails 1, WVS, WVS2, X-Pro-Lys N-terminal protein methyltransferase 1A, enhancer of zeste 2 polycomb repressive complex 2 subunit, hEED