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

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Name:YK-4-279; 
Cat. No. :CS-0667
CAS No. :1037184-44-3
Formula:C17H13Cl2NO4
M. Wt. : 366.20
Solubility:10 mM in DMSO

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 AES-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.

Rahim S, et al. YK-4-279 inhibits ERG and ETV1 mediated prostate cancer cell invasion.PLoS One. 2011 Apr 29;6(4):e19343. Barber-Rotenberg JS, et al. Single enantiomer of YK-4-279 demonstrates specificity in targeting the oncogene EWS-FLI1.Oncotarget. 2012 Feb;3(2):172-82. Erkizan HV, 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.