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Merck
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Key Documents

SML1481

Sigma-Aldrich

FzM1

≥98% (HPLC)

同義詞:

1-(3-Hydroxy-5-(thiophen-2-yl)phenyl)-3-(naphthalen-2-yl)urea

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About This Item

經驗公式(希爾表示法):
C21H16N2O2S
CAS號碼:
分子量::
360.43
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 20 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

O=C(NC1=CC(C=CC=C2)=C2C=C1)NC3=CC(C4=CC=CS4)=CC(O)=C3

InChI

1S/C21H16N2O2S/c24-19-12-16(20-6-3-9-26-20)11-18(13-19)23-21(25)22-17-8-7-14-4-1-2-5-15(14)10-17/h1-13,24H,(H2,22,23,25)

InChI 密鑰

OBTSACXGWYGCPK-UHFFFAOYSA-N

生化/生理作用

FzM1 is an allosteric ligand of the Frizzled4 (Fz4) receptor and a Wnt/β-catenin pathway inhibitor, found by a screen for pharmacological chaperones for a misfolded mutant of the Frizzled4 (Fz4) receptor. FzM1 is believed to induce conformational changes in Fz4 by interacting with the third intracellular loop, ICL3, inhibiting binding of dishevelled (Dsh) and hampering the formation of the Fz4-Dsh complex that is necessary for β-catenin nuclear transport and ultimately transcription of TCF/LEF-regulated genes. FzM1 was tested on two tumor cell lines. U87MG glioblastoma cells acquired a more differentiated phenotype on application. FzM1 and FzM1alk also sped up the differentiation of Caco-2 cells. FzM1 has a log EC50 value of 5.74 for inhibition of Wnt antagonism.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3


分析證明 (COA)

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Serena F Generoso et al.
Nature chemical biology, 11(4), 280-286 (2015-03-10)
Upon binding, ligands can chaperone their protein targets by preventing them from misfolding and aggregating. Thus, an organic molecule that works as folding chaperone for a protein might be its specific ligand, and, similarly, the chaperone potential could represent an

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