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YK 4-279
- Soluble in DMSO
- MF: C17H13Cl2NO4
- MW: 366.2
Description
YK 4-279 is an inhibitor of oncogenic ETS-family transcriptional programs, originally identified for blocking the interaction between EWS-FLI1 and RNA helicase A. It also inhibits ERG-related transcriptional activity in prostate cancer-relevant systems.
EWS-FLI1 and ERG are aberrant transcriptional drivers in Ewing sarcoma and selected prostate cancers. YK 4-279 is useful for studying transcription-factor protein interactions and oncogenic ETS dependency.
Key Features
- EWS-FLI1/RNA helicase A interaction inhibitor
- Reported Kd: 9.48 µM for EWS-FLI1/RHA interaction
- Also inhibits ERG biological activity (reported Kd: 11.7 µM)
- Suppresses ETS-driven tumor-cell phenotypes in reported models
Applications
- Ewing sarcoma pharmacology
- ETS transcription factor research
- Protein-protein interaction inhibitor studies
- Prostate cancer ERG pathway models
More Information
| Parent CAS No. | 1037184-44-3 |
|---|---|
| Chemical Name | 4,7-dichloro-3-hydroxy-3-(2-(4-methoxyphenyl)-2-oxoethyl)indolin-2-one |
| SMILES | N1C2=C(C(Cl)=CC=C2Cl)C(O)(CC(C2=CC=C(OC)C=C2)=O)C1=O |
| MFCD | N.A. |
| InChi | InChI=1S/C17H13Cl2NO4/c1-24-10-4-2-9(3-5-10)13(21)8-17(23)14-11(18)6-7-12(19)15(14)20-16(17)22/h2-7,23H,8H2,1H3,(H,20,22) |
| InChiKey | HLXSCTYHLQHQDJ-UHFFFAOYSA-N |
| CID | 44632017 |
| Short Description | ETV1 inhibitor |
References
- S. Rahim et al. A small molecule inhibitor of ETV1, YK-4-279, prevents prostate cancer growth and metastasis in a mouse xenograft model. PLoS One. 2014 Dec 5;9(12):e114260.
- S. Rahim et al. YK-4-279 inhibits ERG and ETV1 mediated prostate cancer cell invasion. PLoS One. 2011 Apr 29;6(4):e19343.
- H.V. Erkizan et al. A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing's sarcoma. Nat Med. 2009 Jul;15(7):750-6.
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