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YK-4-279 CAS: 1037184-44-3

Category: Inhibitors
Product Name: YK-4-279
Cat No: I000219
CAS No: 1037184-44-3
Synonyms: 4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one
Molecular Formula: C17H13Cl2NO4
Molecular Weight: 366.2
SMILES: ClC1=CC=C(Cl)C(N2)=C1C(O)(CC(C3=CC=C(OC)C=C3)=O)C2=O
InChI: None
InChIKey: HLXSCTYHLQHQDJ-UHFFFAOYSA-N
Solubility: 10 mM in DMSO
Target: ES-FLI1/RHA
Storage: Store at -20°C
CAS 1037184-44-3,YK-4-279
  • Description

YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1. YK-4-279 inhibits Ewing's sarcoma family tumor (ESFT) cell growth; YK-4-279 induces apoptosis.
IC50 value:
Target: RNA Helicase A
ES-FLI1 is an oncogenic fusion protein found in Ewing’s sarcoma, a family of undifferentiated tumors that occur throughout the body. The binding of RNA helicase A (RHA) to ES-FLI1 promotes its oncogenic function. YK-4-279 is an inhibitor of protein-protein interactions between ES-FLI1 and RHA. At 10 μM, YK-4-279 blocks RHA binding to ES-FLI1 and induces apoptosis of a panel of Ewing’s sarcoma tumor cell lines with IC50 values ranging from 0.5-2 μM. At 1.5 mg per dose, YK-4-279 reduces the growth of Ewing’s sarcoma orthotopic xenografts in mice after treatment with the inhibitor for two weeks.

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:YK-4-279 effectively antagonizes EWS-FLI1 induced leukemia in a transgenic mouse model. Minas TZ, Han J, Javaheri T, Hong SH, Schlederer M, Saygideğer-Kont Y, Çelik H, Mueller KM, Temel I, Özdemirli M, Kovar H, Erkizan HV, Toretsky J, Kenner L, Moriggl R, Üren A.Oncotarget. 2015 Nov 10;6(35):37678-94. doi: 10.18632/oncotarget.5520. PMID: 26462019 Free PMC Article
2:An Oral Formulation of YK-4-279: Preclinical Efficacy and Acquired Resistance Patterns in Ewing Sarcoma. Lamhamedi-Cherradi SE, Menegaz BA, Ramamoorthy V, Aiyer RA, Maywald RL, Buford AS, Doolittle DK, Culotta KS, O'Dorisio JE, Ludwig JA.Mol Cancer Ther. 2015 Jul;14(7):1591-604. doi: 10.1158/1535-7163.MCT-14-0334. Epub 2015 May 11. PMID: 25964201 Free Article
3:A small molecule inhibitor of ETV1, YK-4-279, prevents prostate cancer growth and metastasis in a mouse xenograft model. Rahim S, Minas T, Hong SH, Justvig S, Çelik H, Kont YS, Han J, Kallarakal AT, Kong Y, Rudek MA, Brown ML, Kallakury B, Toretsky JA, Üren A.PLoS One. 2014 Dec 5;9(12):e114260. doi: 10.1371/journal.pone.0114260. eCollection 2014. PMID: 25479232 Free PMC Article
4:Single enantiomer of YK-4-279 demonstrates specificity in targeting the oncogene EWS-FLI1. Barber-Rotenberg JS, Selvanathan SP, Kong Y, Erkizan HV, Snyder TM, Hong SP, Kobs CL, South NL, Summer S, Monroe PJ, Chruszcz M, Dobrev V, Tosso PN, Scher LJ, Minor W, Brown ML, Metallo SJ, Üren A, Toretsky JA.Oncotarget. 2012 Feb;3(2):172-82. PMID: 22383402 Free PMC Article
5:YK-4-279 inhibits ERG and ETV1 mediated prostate cancer cell invasion. Rahim S, Beauchamp EM, Kong Y, Brown ML, Toretsky JA, Üren A.PLoS One. 2011 Apr 29;6(4):e19343. doi: 10.1371/journal.pone.0019343. PMID: 21559405 Free PMC Article


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