一般描述
BIX-01294 是一种二氮嗪-喹唑啉胺衍生物，是组蛋白-赖氨酸甲基转移酶 (HMTase) 抑制剂，可调节染色质的表观遗传状态。BIX-01294 抑制组蛋白-3 赖氨酸 (9) 甲基化 (H3K9me) 的 G9aHMTase 依赖性水平。Bix-01294 和组蛋白去乙酰化酶 (HDAC) 抑制剂丙戊酸可分别替代多能干细胞诱导 (iPS) 配方中异位 OCT4 (POU5F1) 和 cMyc 的需求。
应用
BIX 01294 三盐酸盐水合物可用于：
- 作为组蛋白甲基化抑制剂，处理 E4 细胞，分析绿色荧光蛋白（d2EGFP）的表达
- 研究 G9a 在神经母细胞瘤肿瘤生长中的作用
- 作为 G9a 的特异性抑制剂，处理SK-N-AS,、BE(2)-C, SK-N-DZ、 SK-N-F1、K-N-F1和SHEP1神经母细胞瘤细胞系
生化/生理作用
BIX 01294 是一种选择性组蛋白甲基转移酶抑制剂。在抑制组蛋白赖氨酸甲基转移酶时，BIX 01294 不与辅因子 S-腺苷甲硫氨酸竞争。靶酶是 G9a，它在体外选择性损害 G9a HMTase 和 H3K9me2 的生成。
特点和优势
这种化合物是基因调控研究的特色产品。点击此处发现更多特色基因调控产品。在 sigma.com/discover-bsm 可了解更多关于生物活性小分子的其他研究领域。
其他说明
化学探针门户网站已对 BIX-01294 进行了专家评审和推荐。欲了解更多信息，请访问化学探针门户网站上的 BIX-01294 探针摘要。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
Valeria Colicchia et al.
FEBS open bio, 12(10), 1896-1908 (2022-09-06)
The tetracycline repressor (tetR)-regulated system is a widely used tool to specifically control gene expression in mammalian cells. Based on this system, we generated a human osteosarcoma cell line, which allows for the inducible expression of an EGFP fusion of
Lin Lin et al.
Journal of Alzheimer's disease : JAD, 70(4), 1175-1185 (2019-07-20)
Emerging evidence suggests that epigenetic dysregulation of gene expression is one of the key molecular mechanisms of neurodegeneration and Alzheimer's disease (AD). However, little is known about the role of epigenetic dysregulation on synaptic dysfunction in humans, because of the
Inhibition of H3K9 methyltransferase G9a repressed cell proliferation and induced autophagy in neuroblastoma cells
Ke XX, et al.
PLoS ONE, 9(9), e106962-e106962 (2014)
Jian Qin et al.
Oncology letters, 15(6), 9757-9765 (2018-06-22)
Euchromatic histone-lysine N-methyltransferase (G9A), the primary histone methyltransferase for histone H3 Lys9, has been identified to be upregulated in numerous types of cancer. The aim of the present study was to analyze the clinical significance of G9A, and preliminarily explore
Tanel Punga et al.
EMBO molecular medicine, 2(4), 120-129 (2010-04-08)
Friedreich ataxia is a degenerative disease caused by deficiency of the protein frataxin (FXN). An intronic expansion of GAA triplets in the FXN-encoding gene, FXN, causes gene silencing and thus reduced FXN protein levels. Although it is widely assumed that
商品
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