SGC 0946 (SGC0946)是EPZ004777的溴化类似物，一种DOT1L甲基转移酶选择性抑制剂，IC₅₀为0.3 nM，对DNMT1没有作用。DOT1L是催化组蛋白H3赖氨酸79 (H3K79)甲基化的赖氨酸甲基转移酶，SGC0946减少H3K79二甲基化，对白血病和乳腺癌细胞表现出抗癌活性。

参考文献

1.Yu W, et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288.

2.Zhang X, et al. Prognostic and therapeutic value of disruptor of telomeric silencing-1-like (DOT1L) expression in patients with ovarian cancer. J Hematol Oncol. 2017 Jan 23;10(1):29.

3.Zhang L, et al. Inhibition of histone H3K79 methylation selectively inhibits proliferation, self-renewal and metastatic potential of breast cancer. Oncotarget. 2014 Nov 15;5(21):10665-77.

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