FzM1

Names

[ Name ]:
FzM1

[Synonym ]:
Urea, N-[3-hydroxy-5-(2-thienyl)phenyl]-N'-2-naphthalenyl-
FzM1
1-[3-Hydroxy-5-(2-thienyl)phenyl]-3-(2-naphthyl)urea
1-(3-hydroxy-5-(thiophen-2-yl)phenyl)-3-(naphthalen-2-yl)urea

Biological Activity

[Description]:

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; 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.

[References]

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. View Related Products by Target Frizzled

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
518.3±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₁H₁₆N₂O₂S

[ Molecular Weight ]:
360.429

[ Flash Point ]:
267.2±30.1 °C

[ Exact Mass ]:
360.093262

[ LogP ]:
5.29

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.779

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Precautionary Statements ]:
P301 + P312 + P330

[ RIDADR ]:
NONH for all modes of transport

Articles

Pharmacological folding chaperones act as allosteric ligands of Frizzled4.

Nat. Chem. Biol. 11(4) , 280-6, (2015)

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 speci...