生物活性分子抑制剂dTRIM24

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dTRIM24  纯度: 99.69%

dTRIM24 是一种选择性的双功能基于 PROTAC 技术的 TRIM24 降解剂,由von Hippel-LindauTRIM24 两者配体组成。

dTRIM24

dTRIM24 Chemical Structure

CAS No. : 2170695-14-2

规格 价格 是否有货 数量
5 mg ¥3500 In-stock
10 mg ¥5500 In-stock
25 mg ¥13200 In-stock
50 mg ¥24500 In-stock
100 mg ¥42000 In-stock
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500 mg   询价  

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dTRIM24 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24.

IC50 & Target

TRIM24[2].

体外研究
(In Vitro)

dTRIM24 is a degrader of TRIM24 bromodomain. Recruitment of the VHL E3 ubiquitin ligase by dTRIM24 elicits potent and selective degradation of TRIM24. The anti-proliferative consequences of chemical degradation versus inhibition of TRIM24 are assessed. Growth over time is determined for MOLM-13 cells treated with dTRIM24, IACS-9571, VL-269, and eTRIM24. dTRIM24 suppresses growth to a greater extent than does IACS-9571, accompanied by apoptosis measured as enhanced PARP cleavage. In agreement with a sustained proliferative defect observed following dTRIM24 treatment, near-complete degradation of TRIM24 is observed in dTRIM24-treated cells throughout the duration of the experiment[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1113.30

Formula

C55H68N8O13S2

CAS 号

2170695-14-2

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 : 100 mg/mL (89.82 mM; Need ultrasonic)

Ethanol : < 1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8982 mL 4.4912 mL 8.9823 mL
5 mM 0.1796 mL 0.8982 mL 1.7965 mL
10 mM 0.0898 mL 0.4491 mL 0.8982 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: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.25 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.25 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (2.25 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.25 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Gechijian LN, et al. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat Chem Biol. 2018 Apr;14(4):405-412.

Cell Assay
[2]

MOLM-13 cells are seeded at 30,000 cells/well. Growth over time of MOLM-13 cells treated with 5 μM of indicated compounds (e.g., dTRIM24) over 7 d. At endpoints, cells are suspended and mixed with Viacount reagent at 1:3. The mixture is incubated for 5 min, and viable cells are counted on the Guava easycyte flow cytometer. Means from three technical replicates of cell counts are calculated[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Gechijian LN, et al. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat Chem Biol. 2018 Apr;14(4):405-412.

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