FzM1

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].

Product Specifications

CAS Number

[1680196-54-6]

Product Name Alternative

Disodium (R)-2-hydroxyglutarate,ICI-118560

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Wnt; β-catenin

Type

Reference compound

Related Pathways

Stem Cell/Wnt

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/fzm1.html

Purity

98.72

Solubility

DMSO : 62.5 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC2=CC=CC=C2C=C1)NC3=CC(O)=CC(C4=CC=CS4)=C3

Molecular Formula

C21H16N2O2S

Molecular Weight

360.43

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.