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FzM1

Chemical Structure : FzM1

CAS No.: 1680196-54-6

FzM1 (Fzd4 modulator FzM1;FzM 1)

Catalog No.: PC-60976Not For Human Use, Lab Use Only.

FzM1 is a negative allosteric modulator of the Frizzled4 (Fzd4) receptor and a Wnt/β-catenin pathway inhibitor with pEC50 value of 5.74 for inhibition of Wnt antagonism.

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Biological Activity

FzM1 is a negative allosteric modulator of the Frizzled4 (Fzd4) receptor and a Wnt/β-catenin pathway inhibitor with pEC50 value of 5.74 for inhibition of Wnt antagonism.
FzM1 induces 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.

Physicochemical Properties

M.Wt 360.43
Formula C21H16N2O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Generoso SF, et al. Nat Chem Biol. 2015 Apr;11(4):280-6.

2. Riccio G, et al. Biochemistry. 2018 Jan 2. doi: 10.1021/acs.biochem.7b01087.

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