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FzM1.8 is a small molecule, allosteric agonist of the Frizzled receptor Fzd4 with pEC50 of 6.4, potentiates β-catenin pathway in the absence of any WNT ligand; biases FZD4 signaling toward a FZD4/PI3K axis that culminates into transactivation of β-catenin/TCF activity by the histone acetyltransferase CBP/p300; preserves stemness and promotes proliferation of undifferentiated cells.


SRI 37892


SRI 37892 (SRI37892) is a novel potent, small molecule Frizzled 7 (Fzd 7) inhibitor with IC50 of 0.66 uM in Wnt/β-catenin assay; also displays potent activity against Wnt/β-catenin signaling in LRP6-expressing HEK293 cells with IC50 of 0.78 uM, demonstrates potent activity against breast cancer HS578T and BT549 cell proliferation with IC50 of 2.2 and 1.9 uM, respectively; targets Fzd7 transmembrane domain (TMD) and bolcks Wnt/Fzd7 signaling.


Peptide Fz7-21

Peptide Fz7-21 is a potent, selective peptide inhibitor of Frizzled 7 receptor, inhibits exogenous WNT3A stimulated Wnt-β-catenin signaling in HEK293 cells with IC50 of 100 nM; also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells with IC50 of 50 nM; shows isoform-selective binding to the Fc-tagged FZD1, FZD2 and FZD7 CRDs with EC50 of 19-58 nM, whereas little to no binding to the FZD4, FZD5, FZD8, FZD9 or FZD10 CRDs; impaires Wnt signaling in cultured cells and stem cell function in intestinal organoids.


1680196-54-6 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.


150068-95-4 A novel small molecule Wnt signaling inhibitor that targets the cysteine-rich domain of Frizzled, specifically binds to the Wnt binding site on the Frizzled8 cysteine-rich domain with Kd of 2.9 uM, IC50 of 5.7 uM.

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