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Merck
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主要文件

SML1817

Sigma-Aldrich

BCI-121

≥98% (HPLC)

别名:

4-(Aminocarbonyl)-N-(4-bromophenyl)-1-piperidineacetamide, BCI121

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About This Item

经验公式（希尔记法）:
C14H18BrN3O2
CAS号:
432529-82-3
分子量:
340.22
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 20 mg/mL, clear

儲存溫度

2-8°C

生化／生理作用

BCI-121 是一种底物竞争性 SMYD3 抑制剂，可降低核组蛋白 H3 lys4 二甲基化和三甲基化的级别（通过HT29 细胞中 50%/H3K4me2 和 40%H3K4me3；48小时内100μM BCI-121实现），下调已知的 SMYD3 靶基因转录，并选择性影响 SMYD3 依赖的癌症培养物增殖（46%/HT29 和 54%/HCT116 增殖减少；72小时内的100μM BCI-121），对低表达 SMYD3 的癌细胞几乎没有抗增殖作用。BCI-121 通过直接亲和作用靶向 SMYD3（kon 357.7/M/s；k off 4.23 × 10 -3 /s；K D = K off/ K on = 11.8μM），并与组蛋白结合 SMYD3（% 抑制率/[组蛋白H4 肽]:[BCI-121] 比值 = 36.5%/1：1 和 51.0%/1：2.5）有效竞争。
BCI121能够减少MDA-MB-231细胞的间充质特征。它还可以降低它们体外和体内的入侵能力。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

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Protein methylation is one of the important post-translational modifications. Although its biological and physiological functions were unknown for a long time, we and others have characterized a number of protein methyltransferases, which have unveiled the critical functions of protein methylation
SMYD3 promotes the epithelial-mesenchymal transition in breast cancer
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The coordinated expression of myogenic regulatory factors, including MyoD and myogenin, orchestrates the steps of skeletal muscle development, from myoblast proliferation and cell-cycle exit, to myoblast fusion and myotubes maturation. Yet, it remains unclear how key transcription factors and epigenetic
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Journal of cellular physiology, 230(10), 2447-2460 (2015-03-03)
SMYD3 is a histone lysine methyltransferase that plays an important role in transcriptional activation as a member of an RNA polymerase complex, and its oncogenic role has been described in different cancer types. We studied the expression and activity of

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