2. Epigenetics
  3. Epigenetic Reader Domain Histone Acetyltransferase
  4. GNE-049

GNE-049 是一种高效的选择性 CBP 抑制剂，在 TR-FRET 实验中 IC50 为 1.1 nM。GNE-049 还抑制 BRET 和 BRD4(1)，IC50 分别为 12 nM 和 4200 nM。

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GNE-049

GNE-049 Chemical Structure

CAS No. : 1936421-41-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1112
In-stock
5 mg ￥990
In-stock
10 mg ￥1585
In-stock
25 mg ￥2395
In-stock
50 mg ￥4050
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

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GNE-049 相关抗体

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CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively[1].

IC50 & Target

CBP/p300

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
12 nM
Compound: 10
Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated human CBP expressed in HEK293 cells after overnight incubation by BRET assay
Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated human CBP expressed in HEK293 cells after overnight incubation by BRET assay
[PMID: 28892380]
体外研究
(In Vitro)

选择 GNE-049 进行进一步分析，是因为它在肝微粒体 (LM) 稳定性、选择性和细胞效力之间达到了最佳平衡。GNE-049 在 BRET 细胞测定中表现出色，并且在靶标参与的正交测量中，GNE-049 显示出可抑制 MYC (MV4-11 细胞系) 的表达，EC50 为 14 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GNE-049 相关抗体:
体内研究
(In Vivo)

GNE-049 在小鼠、大鼠、犬和猴体内均表现出可接受的药代动力学 (PK)。对多种溴结构域的效力测定表明，GNE-049 对 CBP/P300 具有选择性，更重要的是，其对 BRD4(1) 的选择性相当高 (高出 3820 倍)。在大鼠单剂量 (30-250 mg/kg QD) 毒代动力学研究中进一步评估了 GNE-049。在 250 mg/kg 剂量水平下，在数只大鼠中观察到中枢神经系统 (CNS) 相关不良症状 (例如明显的过度活跃和发声)。此外，在 250 mg/kg 剂量水平下，给药后 3 小时脑内游离药物浓度与血浆内游离药物浓度 (Kp,uu) 之比确定为 0.43，这表明 GNE-049 正在渗透到中枢神经系统并可能导致观察到的毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

510.58

Formula

C27H32F2N6O2
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (195.86 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9586 mL 9.7928 mL 19.5856 mL
5 mM 0.3917 mL 1.9586 mL 3.9171 mL
查看完整储备液配制表

* 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 (stored under nitrogen)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Animal Administration
[1]

Mice[1]
Twelve female CD-1 mice are used. All animals are 6-9 weeks old at the time of study and weighed between 20 and 35 g. Animals (n=3 per dosing route) are dosed with GNE-049 or GNE-781 at 1 mg/kg iv (in propyl ethylene glycol 400 (35% v/v) and water (65% v/v)) or 5 mg/kg po (suspended in 0.5% w/v methylcellulose, 0.2% w/v Tween 80). Food and water are available ad libitum to all animals. Serial blood samples (15 μL) are collected by tail nick at 0.033, 0.083, 0.25, 0.5, 1, 3, 8, and 24 h after the intravenous administration and 0.083, 0.25, 0.5, 1, 3, 8, and 24 h after the oral administration. All blood samples are diluted with 60 μL of water containing 1.7 mg/mL EDTA and kept at -80 °C until analysis[1].
Rats[1]
Twelve male Sprague-Dawley rats are used. All animals are 6-9 weeks old at the time of study and weighed between 200 and 300 g. Animals (n=3 per dosing route) are dosed with GNE-049 or GNE-781 at 1 mg/kg iv (in propyl ethylene glycol 400 (35% v/v) and water (65% v/v)) or 5 mg/kg po (suspended in 0.5% w/v methylcellulose, 0.2% w/v Tween 80). Food and water are available ad libitum to animals in the iv groups. Animals in po groups are fasted overnight and food withheld until 4 h postdose. Approximately 250 μL of blood are collected via the catheter at 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 8, and 24 h after the intravenous or oral administration. All blood samples are collected into tubes containing 5 μL of 0.5 M K2EDTA and processed for plasma. Samples are centrifuged (2500g for 15 min at 4°C) within 1 h of collection, and plasma samples are kept at -80 °C until analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

GNE-049 相关分类

完整储备液配制表

* 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 (stored under nitrogen)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9586 mL 9.7928 mL 19.5856 mL 48.9639 mL
5 mM 0.3917 mL 1.9586 mL 3.9171 mL 9.7928 mL
10 mM 0.1959 mL 0.9793 mL 1.9586 mL 4.8964 mL
15 mM 0.1306 mL 0.6529 mL 1.3057 mL 3.2643 mL
20 mM 0.0979 mL 0.4896 mL 0.9793 mL 2.4482 mL
25 mM 0.0783 mL 0.3917 mL 0.7834 mL 1.9586 mL
30 mM 0.0653 mL 0.3264 mL 0.6529 mL 1.6321 mL
40 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2241 mL
50 mM 0.0392 mL 0.1959 mL 0.3917 mL 0.9793 mL
60 mM 0.0326 mL 0.1632 mL 0.3264 mL 0.8161 mL
80 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.6120 mL
100 mM 0.0196 mL 0.0979 mL 0.1959 mL 0.4896 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNE-0491936421-41-8GNE049GNE 049Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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