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The key mediator of Wnt signaling is the transcriptional co-activator b-catenin. In the cytoplasm, b-catenin is tightly bound to a complex that includes Axin and GSK-3b. Stimulation causes b-catenin stabilization, translocation to the nucleus and association with TCF4 to initiate transcription of responsive genes, referred to as Catenin Responsive Transcription (CRT). Virtually all Wnt-associated cancers are the result of misregulated CRT. Three inhibitors of CRT (iCRT) were identified in a screen that employed RNAi based knockdown of Axin, which stimulates CRT without affecting upstream mechanisms such as GSK activity, transduction by disheveled / frizzled, etc. These compounds are potent inhibitors of CRT reporter genes, as well as endogenous gene targets. The compounds also disrupt b-catenin-TCF4 interaction in a dose dependent manner, and cause G0/G1 arrest in colon tumor lines.
| Molecular Weight | 394.53 |
| Formula | C23H26N2O2S |
| CAS Number | 901751-47-1 |
| Form | Solid |
| Solubility (25°C) | DMSO: ≥5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Wnt/beta-catenin Products |
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(9Z,12Z,15Z)-N-[(3-Methoxyphenyl)methyl]-9,12,15-octadecatrienamide is a macamide isolated from Maca (Lepidium meyenii Walp). (9Z,12Z,15Z)-N-[(3-Methoxyphenyl)methyl]-9,12,15-octadecatrienamide induces mesenchymal stem cells osteogenic differentiation and consequent bone formation through activating the canonical Wnt/β‐catenin signaling pathway. |
| F7H
F7H is a Frizzled receptor FZD7 antagonist with IC50 of 1.25 μM. F7H is a potent ligand for the FZD7 transmembrane domain (TMD). |
| UU-T02
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| Calphostin C
Calphostin C (PKF115-584) is a small molecule inhibitor of Wnt/beta-catenin/lef-1 signaling. Calphostin C is also a potent and specific inhibitor of protein kinase C. PKF115-584 efficiently killed CLL cells (LC(50)<1 microM), whereas normal B cells were not significantly affected. |
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