1680196-54-6
1680196-54-6
Chemical Structure
FzM1
- CAS No.: 1680196-54-6
- Formula:C21H16N2O2S
- Molecular Weight:360.43
IUPAC Name: 1-(3-hydroxy-5-(thiophen-2-yl)phenyl)-3-(naphthalen-2-yl)urea
InChIKey: OBTSACXGWYGCPK-UHFFFAOYSA-N
SMILES: O=C(NC1=CC2=CC=CC=C2C=C1)NC3=CC(O)=CC(C4=CC=CS4)=C3
Biological Activity: FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=?6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade[1][2].
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FzM1 | 98.72% | FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=?6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade. | ||||||||||||||||||||
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References
- [1]. Gennaro Riccio, et al. A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist. Biochemistry. 2018 Feb 6;57(5):839-851. [Content Brief]
- [2]. Hong Y, et al. Effects of RAGE-Specific Inhibitor FPS-ZM1 on Amyloid-β Metabolism and AGEs-Induced Inflammation and Oxidative Stress in Rat Hippocampus. Neurochem Res. 2016 May;41(5):1192-9. [Content Brief]
