YK-4-279

• CAT Number: I000219
• CAS Number: 1037184-44-3
• Molecular Formula: C₁₇H₁₃Cl₂NO₄
• Molecular Weight: 366.2
• Purity: ≥95%
• Target: ES-FLI1/RHA
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• 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
• SMILES: COC1=CC=C(C=C1)C(=O)CC2(C3=C(C=CC(=C3NC2=O)Cl)Cl)O

YK-4-279(CAT: I000219) is a small-molecule inhibitor that specifically targets the Ewing’s sarcoma breakpoint family member 1 (EWS-FLI1) fusion protein. EWS-FLI1 is an oncogenic transcription factor formed as a result of chromosomal translocation in Ewing’s sarcoma, a type of cancer commonly found in bone and soft tissues. YK-4-279 has shown promising anti-tumor activity in preclinical studies and is being investigated as a potential therapeutic agent for Ewing’s sarcoma. By inhibiting the activity of EWS-FLI1, YK-4-279 aims to disrupt the oncogenic signaling pathways and inhibit the growth of Ewing’s sarcoma cells.

Reference

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 Article2: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 Article3: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 Article4: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 Article5: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