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iCRT14
- CRT Inhibitor iCRT14
- Soluble in DMSO
- MF: C21H17N3O2S
- MW: 375.44
Description
Small-molecule inhibitor of the Wnt/wingless signaling pathway (IC50 value 40 nM in a Wnt responsive STF16-luc reporter assay) that antagonizes the transcriptional function of nuclear β-catenin, and inhibits direct interactions between β-cat and TCF4. iCRT 14 exhibits specific cytotoxicity towards human colon tumor biopsy cultures as well as colon cancer cell lines that exhibit deregulated Wnt signaling. Similar mode of action as iCRT5 (Axon 2133)
More Information
| Parent CAS No. | 677331-12-3 |
|---|---|
| Chemical Name | 5-((2,5-dimethyl-1-(pyridin-3-yl)-1H-pyrrol-3-yl)methylene)-3-phenylthiazolidine-2,4-dione |
| SMILES | S1/C(=CC2C=C(C)N(C3=CC=CN=C3)C=2C)/C(=O)N(C2=CC=CC=C2)C1=O |
| MFCD | MFCD04366833 |
| InChi | InChI=1S/C21H17N3O2S/c1-14-11-16(15(2)23(14)18-9-6-10-22-13-18)12-19-20(25)24(21(26)27-19)17-7-4-3-5-8-17/h3-13H,1-2H3/b19-12- |
| InChiKey | NCSHZXNGQYSKLR-UNOMPAQXSA-N |
| CID | 5967294 |
| 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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