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Argonaute-2 Inhibitor, BCI-137-Calbiochem

品牌
Sigma-Aldrich
货号
5.31552
规格纯度
A cell-permeable compound that directly and reversibly interacts with miRNA binding domain of Argonaute-2 (Kd = 126 μM) and inhibits binding of miR-20a, miR-26a, miR-107, miR-223 &let-7a to Ago2.
参考价格
2490.59 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

A cell-permeable dioxotetrahydroquinoxaline compound that mimics uridine monophosphate for affinity interaction at the Argonaute-2 (Ago2) Mid domain (KD = 126 µM) and effectively inhibits Ago2 cellular miRNA loading in acute promyelocytic leukemia (APL) NB4 cultures (% inhibition by RIP = 79%/miR-107, 73%/let-7a, 73%/miR-223, 68%/miR-26a, 53%/miR-60a; 100 nM for 48 h) without affecting cellular Ago2 stability. Consistent with the involvement of Ago2 in heterochromatic miR-155HG silencing, BCI-137 is reported to decrease miR-155HG promoter region-associated Ago2 with a concomitant acetylation induction of the promoter region-associated histone H4 (70% reduced Ago2 association and 300% enhanced H4 acetylation, respectively, by ChIP; 10 µM). Likewise, Ago2 inhibition by BCI-137 is shown to boost Retinoic Acid-(RA, Cat. no. 554720) induced NB4 granulocyte differentiation as a result of greatly upregulated expression of the differentiation-related miRNAs (140% and 255% increased miR-26a and miR-223 level, respectively, compared to 100 nM RA stimulation alone for 96 h) without affecting NB4 proliferation or viability (up to 10 µM and 96 h with or without 100 nM RA stimulation).
A cell-permeable, non-toxic dioxotetrahydroquinoxaline compound that mimics uridine and directly and reversibly interacts with the microRNA (miRNA) binding domain of Argonaute-2 (Ago2; KD = 126 µM) and significantly inhibits binding of miR-20a, miR-26a, miR-107, miR-223, and let-7a to Ago2. However, it does not affect Ago2 stability in cells. Displaces Ago2 from the miR-155 host gene promoter region (70% reduction in Ago2 association) and increases histone H4 acetylation (~300%) in NB4 leukemia cell line. Promotes retinoic acid-induced differentiation of NB4 cells to granulocytes.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化/生理作用

Cell permeable: yes
Primary Target
Argonaute-2
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Masciarelli, S., et al. 2014. ACS Chem. Biol.9, 1674.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C11H11N3O6S
分子量313.29

产品性质

质量水平100
测定≥97% (HPLC)
形式solid
效能126 μM Kd
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 gray-white
溶解性DMSO: 100 mg/mL
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

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