BRD4770
目录号 : KM9996 CAS No. : 1374601-40-7 纯度 : 98%

BRD4770 是一种组蛋白甲基转移酶 G9a 抑制剂。BRD4770 可抑制 H3K9 的二甲基和三甲基化,EC50 为 5 µM,对 H3K27me3,H3K36me3,H3K4me3 和 H3K79me3 几乎没有影响。BRD4770 可以激活共济失调毛细血管扩张突变 (ATM) 途径并诱导细胞衰老。

规格 价格 是否有货 数量
10mg
In-stock
50mg
In-stock
100mg
In-stock
500mg
In-stock
1g 询价 In-stock
5g 询价 In-stock

Other Forms of Rapamycin:

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生物活性

BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 µM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence.

体外研究

BRD4770 (0-20 µM; 72 hours; PANC-1 cells) treatment reduces the number of cells after 72 h.
BRD4770 (2.5-5 µM; 24 hours; PANC-1 cells) treatment decreases H3K9 trimethylation level by 23% in PANC-1 cells.
BRD4770 induces a senescent phenotype in a pancreatic cancer cell line. BRD4770 also inhibits both anchorage-dependent and -independent cell proliferation and induces G2/M cell-cycle arrest. BRD4770 activates the ataxia telangiectasia mutated (ATM) pathway without inducing DNA damage, while the ataxia telangiectasia and Rad3-related protein (ATR) pathway is not affected.
BRD4770 also induces increased levels of lysine acetylation in cells without inhibiting histone deacetylases.

Cell Viability Assay

Cell Line: PANC-1 cells
Concentration: 0 µM, 0.625 µM, 1.25 µM, 2.5 µM, 5 µM, 10 µM, 20 µM
Incubation Time: 72 hours
Result: Reduced the number of cells after 72 h.

Western Blot Analysis

Cell Line: PANC-1 cells
Concentration: 2.5 µM, 5 µM
Incubation Time: 24 hours
Result: Decreased H3K9 trimethylation level by 23% in PANC-1 cells.
分子式
C25H23N3O3
分子量
413.47
CAS号
1374601-40-7
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (80.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4186 mL 12.0928 mL 24.1856 mL
5 mM 0.4837 mL 2.4186 mL 4.8371 mL
10 mM 0.2419 mL 1.2093 mL 2.4186 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 0.5% Methylcellulose/saline water

    Solubility: 6.25 mg/mL (15.12 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.05 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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