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TCH-165

Cat. No. 7489 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Enhancer of 20S proteasome assembly and 20S-mediated protein degradation
别名： TCH165
化学名： Ethyl (4R,5R)-rel-1-benzyl-5-(4-(benzylamino)phenyl)-2-(4-methoxyphenyl)-4-phenyl-4,5-dihydro-1H-imidazole-4-carboxylate
纯度： ≥98% (HPLC)
说明书
引用文献
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文献 (2)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for TCH-165

TCH-165 is an enhancer of 20S proteasome assembly. TCH-165 regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation. TCH-165 enhances the proteolytic activity of the 20S proteasome by increasing substrate accessibility to the 20S catalytic chamber through 20S gate opening. 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. TCH-165 enhances c-MYC degradation by the 20S proteasome, which reduces c-MYC levels in vivo, and is effective in bortezomib (Cat. No. 7282) resistant cells. TCH-165 down-regulates c-MYC target genes and inhibits cancer cell proliferation and tumor growth in vivo.

技术数据 for TCH-165

分子量 595.74
公式 C39H37N3O3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1446350-60-2
PubChem ID 71762768
InChI Key XXDLWRCUPASJGY-AEGYFVCZSA-N
Smiles CCOC([C@@]1(C2=CC=CC=C2)[C@@H](C3=CC=C(C=C3)NCC4=CC=CC=C4)N(C(C5=CC=C(C=C5)OC)=N1)CC6=CC=CC=C6)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for TCH-165

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
ethanol 59.57 100
DMSO 59.57 100

制备储备液 for TCH-165

以下数据基于产品分子量 595.74。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1.68 mL 8.39 mL 16.79 mL
5 mM 0.34 mL 1.68 mL 3.36 mL
10 mM 0.17 mL 0.84 mL 1.68 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

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参考文献 for TCH-165

参考文献是支持产品生物活性的出版物。

Azevedo et al (2013) Inhibition of the human proteasome by imidazoline scaffolds. J.Med.Chem. 56 10.1021 PMID: 23789888

Njomen et al (2020) Enhancing c-MYC degradation via 20S proteasome activation induces in vivo anti-tumor efficacy. BioRxiv- not yet peer reviewed

Njomen et al (2018) Small molecule modulation of proteasome assembly. Biochemistry 57 4214 PMID: 29897236

If you know of a relevant reference for TCH-165, please let us know.

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关键词: TCH-165, TCH-165 supplier, TCH165, enhancers, enhances, 20S, proteasomes, assembly, modulators, activators, c-myc, Proteasome, 7489, Tocris Bioscience

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This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

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Targeted Protein Degradation Poster

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