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。
生物活性 | TCH-165 is a small molecule modulator ofproteasomeassembly, which increases20Slevels and facilitates20S-mediated protein degradation[1]. |
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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].
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 IC50of 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. |
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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 |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(419.65 mM;Need ultrasonic) 配制储备液 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。 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本网站选购。
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