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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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| XAV939
XAV939 is a potent, cell-permeable small molecule inhibitor of the Wnt/β-catenin pathway to TNKS1 and TNKS2 with IC50 values of 11 and 4 nM respectively. |
| ICG-001
ICG-001 is a novel small molecule inhibitor of TCF/beta-catenin-mediated transcription. ICG-001 specifically binds to cyclic AMP response element-binding protein with an IC50 of 3 μM. |
| IWP-2
IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 27 nM. |
| IWP-L6
IWP-L6 is a highly potent Porcn inhibitor with EC50 of 0.5 nM. |
| IWR-1-endo
IWR-1 (endo-IWR 1) is a Wnt pathway inhibitor with IC50 of 180 nM, induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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