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Merck
CN

SML3911

TCH-165

≥98% (HPLC)

别名:

Ethyl (4R,5R)-rel-1-benzyl-5-(4-(benzylamino)phenyl)-2-(4-methoxyphenyl)-4-phenyl-4,5-dihydro-1H-imidazole-4-carboxylate, rel-Ethyl (4R,5R)-4,5-dihydro-2-(4-methoxyphenyl)-4-phenyl-1-(phenylmethyl)-5-[4-[(phenylmethyl)amino]phenyl]-1H-imidazole-4-carboxylate

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关于此项目

经验公式(希尔记法):
C39H37N3O3
化学文摘社编号:
分子量:
595.73
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

SMILES string

N2([C@@H]([C@](N=C2c6ccc(cc6)OC)(c5ccccc5)C(=O)OCC)c3ccc(cc3)NCc4ccccc4)Cc1ccccc1

InChI

1S/C39H37N3O3/c1-3-45-38(43)39(33-17-11-6-12-18-33)36(31-19-23-34(24-20-31)40-27-29-13-7-4-8-14-29)42(28-30-15-9-5-10-16-30)37(41-39)32-21-25-35(44-2)26-22-32/h4-26,36,40H,3,27-28H2,1-2H3/t36-,39-/m1/s1

InChI key

XXDLWRCUPASJGY-AEGYFVCZSA-N

Biochem/physiol Actions

Cell-permeable and potent activator of 20S proteasome assembly that and enhances 20S-mediated proteolysis.

TCH-165 is a cell-permeable and potent activator of 20S proteasome assembly that favors a proteolytically active, open-gate 20S proteasome subcomplex and enhances 20S-mediated proteolysis (nearly 10-fold ≤1.5 µM) to the detriment of the 26S proteasome, in a time- and dose-dependent manner. TCH-165 restores proteostasis and enhances degradation of intrinsically disordered proteins (IDPs) both in purified protein assays and in cell culture (α-synuclein, tau441, c-MYC, cFos, ornithine decarboxylase). TCH 165 degrades SNAP29 and syntaxin 17 and reduces autophagosome-lysosome fusion. TCH165 inhibits cancer cell proliferation, impedes in vivo tumor growth, and offers neuroprotection from distinct dipeptide repeat (DPR) protein toxicity and is well tolerated in vivo (in mice and in dogs) at therapeutic concentrations.


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



历史批次信息供参考:

分析证书(COA)

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