TCH-165

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TCH-165  纯度: 99.31%

TCH-165 是蛋白酶体组装的小分子调节剂，可增加 20S 水平并促进 20S 介导的蛋白质降解。

TCH-165

TCH-165 Chemical Structure

CAS No. : 1446350-60-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3801 In-stock
5 mg ￥2900 In-stock
10 mg ￥4600 In-stock
50 mg ￥13000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

TCH-165 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Ubiquitination Compound Library
  • Targeted Diversity Library

生物活性

TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation[1].

IC50 & Target

Proteasome assembly[1]
体外研究
(In Vitro)

TCH-165 (0.01-10 μM; 72 hours; RPMI8226 and U87MG cells) treatment inhibits cell growth of RPMI8226 and U87MG cells with IC50 of 1.6 μM and 2.4 μM, respectively[1].
TCH-165 (0-10 μM; 24 hours; HEK293T cells) treatment enhances ODC degradation is blocked by BTZ indicated that this event is proteasome-mediated. TCH-165 enhances proteolytic degradation in a concentration-dependent manner[1].
TCH-165 enhances the chymotrypsin-like (CT-L), trypsin-like (Tryp-L) and caspase-like (Casp-L) activities with EC50s of 4.2 μM, 3.2 μM and 4.7 μM, respectively[1].
TCH-165 enhances 20S-mediated degradation of IDPs, α-syn, and tau in vitro, and does not induce the degradation of structured proteins such as GAPDH[1].
TCH-165-treated cells display a decrease in the assembled 26S and an increase in the 20S proteasome. TCH-165 regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation[1].

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.

Cell Viability Assay[1]

Cell Line: RPMI8226 and U87MG cells
Concentration: 0.01-10 μM
Incubation Time: 72 hours
Result: Inhibited cell growth of RPMI8226 and U87MG cells with IC50 of 1.6 μM and 2.4 μM, respectively.

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 0 μM, 3 μM, 10 μM
Incubation Time: 24 hours
Result: Enhanced proteolytic degradation in a concentration-dependent manner.

分子量

595.73

Formula

C39H37N3O3
CAS 号

1446350-60-2
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 : 250 mg/mL (419.65 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6786 mL 8.3931 mL 16.7861 mL
5 mM 0.3357 mL 1.6786 mL 3.3572 mL
10 mM 0.1679 mL 0.8393 mL 1.6786 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: ≥ 6.25 mg/mL (10.49 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (10.49 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 62.5 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: ≥ 6.25 mg/mL (10.49 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (10.49 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 62.5 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]. Njomen E, et al. Small Molecule Modulation of Proteasome Assembly. Biochemistry. 2018 Jul 17;57(28):4214-4224.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务