| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C21H16N2O2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
FzM1 is a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, reducing WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh = 6.2). It binds an allosteric site in intracellular loop 3 (ICL3) of FZD4, altering the receptor's conformation and thereby inhibiting the WNT/β-catenin cascade[1][2]. It is supplied as a white to light brown solid (C21H16N2O2S, MW 360.43) at 98.72% purity.
Physical & Chemical Properties
| CAS Number | 1680196-54-6 |
|---|---|
| Molecular Formula | C21H16N2O2S |
| Molecular Weight | 360.43 g/mol |
| Purity | 98.72% |
| Appearance | Solid |
| Color | White to light brown |
| SMILES | O=C(NC1=CC2=CC=CC=C2C=C1)NC3=CC(O)=CC(C4=CC=CS4)=C3 |
| Signaling Pathway | Stem Cell/Wnt |
| Solubility | In Vitro: DMSO: 62.5 mg/mL (173.40 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 62.5 mg/mL (173.40 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | 2.08 mg/mL (5.77 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.08 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.08 mg/mL (5.77 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.08 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
FzM1 is a negative allosteric regulator of FZD4 in HEK293 cells co-transfected with FZD4 and a WNT reporter construct; it inhibits the WNT/β-catenin pathway without raising the activity of that WNT reporter construct[1]. Decreased cell viability resulted from FzM1 (15 μM; 24 h, 48 h) treatment in CaCo-2 cells[1]. FzM1 also acts as a negative allosteric regulator of FZD4 signaling initiated by WNT5A in HEK293 cells expressing FZD4, and thereby reduces WRE activity that depends on WNT5A[1].
Cell Viability Assay[1]
| Cell Line | HEK293 cells |
|---|---|
| Concentration | 15 μM |
| Incubation Time | 24 h, 48 h |
| Result | Decreased the cell viability of HEK293 cells expressing FZD4. Did not increase the activity of the WNT reporter construct, indicating its inhibitory effect on the WNT/β-catenin pathway. |
In Vivo
Wistar rats with AGEs-RAGE activation given FPS-ZM1 (1 mg/kg/d; intraperitoneal injection; once a day; 4 weeks) showed reduced production of Aβ1-40 and Aβ1-42 in the hippocampus, an inhibited increase in Aβ metabolism-related proteins (RAGE, BACE1 and APP), downregulated expression of proinflammatory cytokines (p-NF-κB, TNF-α and IL-1β), an upregulated antioxidant defense system (lower ROS and LPO levels; higher GSH content, SOD activity and GPx activity), and alleviation of AGEs-induced memory impairment[1].
| Animal Model | AGEs-RAGE-activated (intrahippocampal injection) rat model in Wistar rats (male, 6 weeks old)[1] |
|---|---|
| Dosage | 1 mg/kg/d |
| Administration | Intraperitoneal injection, once daily, for 4 weeks |
| Result | Reduced the levels of Aβ1-40 and Aβ1-42 in the hippocampus of rats. Inhibited the increased expressions of Aβ metabolism-related proteins (RAGE, BACE1, and APP), pro-inflammatory cytokines (p-NF-κB, TNF-α, and IL-1β) induced by AGEs. Upregulated the antioxidant defense system, with reduced levels of ROS and LPO, and increased content of GSH, and activities of SOD and GPx. Also, alleviated the memory impairment of rats induced by AGEs, as shown by a significant decrease in the escape latency in the Morris water maze test. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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