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iCRT5
- CRT Inhibitor iCRT5
- Soluble in DMSO
- MF: C16H17NO5S2
- MW: 367.44
Description
iCRT5 is a potent, cell-permeable inhibitor of β-catenin-responsive transcription (CRT) with a reported IC50 value of 18 nM in a Wnt-responsive STF16 luciferase assay. It acts by disrupting β-catenin/TCF-mediated transcriptional output.
Aberrant Wnt/β-catenin signaling contributes to developmental disorders, stem-cell fate changes and multiple cancers. iCRT5 is a useful pharmacological tool for suppressing downstream Wnt transcription rather than upstream ligand or receptor signaling.
Key Features
- Potent inhibitor of β-catenin-responsive transcription
- Cell-permeable Wnt pathway tool compound
- Blocks β-catenin/TCF transcriptional output
- Active in Wnt-responsive reporter assays
Applications
- Wnt/β-catenin pathway research
- TCF reporter assay development
- Cancer signaling studies
- Stem cell and developmental biology models
More Information
| Parent CAS No. | 18623-44-4 |
|---|---|
| Chemical Name | 4-(5-(3,4-dimethoxybenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)butanoic acid |
| SMILES | S1/C(=CC2=CC=C(OC)C(OC)=C2)/C(=O)N(CCCC(O)=O)C1=S |
| MFCD | MFCD00703657 |
| InChi | InChI=1S/C16H17NO5S2/c1-21-11-6-5-10(8-12(11)22-2)9-13-15(20)17(16(23)24-13)7-3-4-14(18)19/h5-6,8-9H,3-4,7H2,1-2H3,(H,18,19)/b13-9- |
| InChiKey | IJWKSBPTJQMUHJ-LCYFTJDESA-N |
| CID | 1416325 |
| Short Description | CRT inhibitor |
References
- FC Gonsalves et al. An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway. Proc Natl Acad Sci USA 2011, 108, 5954-5963.
- BA Narayanan et al. Antagonistic Effect of Small-molecule Inhibitors of Wnt/β-catenin in Multiple Myeloma. Anticancer Res. 2012, 32(11), 4697-4707.
- JN Anastas & RT Moon. WNT signalling pathways as therapeutic targets in cancer. Nat. Rev. Cancer 2013, 13, 11-26.
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