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YK-4-279
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
YK-4-279图片
CAS NO:1037184-44-3
规格:98%
分子量:366.2
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议

产品介绍
RNA Helicase A (RHA) inhibitor
CAS:1037184-44-3
分子式:C17H13Cl2NO4
分子量:366.2
纯度:98%
存储:Store at -20°C

Background:

YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1.


EWS-FLI1 is a disordered protein that precludes standard structure-based small-molecule inhibitor design. EWS-FLI1 binding to RNA helicase A (RHA) is important for its oncogenic function.


In vitro: ESFT cells treated with YK-4-279 showed a dissociation of EWS-FLI1 from RHA by 10 mM, consistent with the KD value. The EWS-FLI1–transfected cells showed a dose-dependent decrease in promoter activity when treated for 18 h with 3 mM and 10 mM YK-4-279. YK-4-279 was relatively specific for ESFT cells as compared to the nontransformed HEK293 cells [1].


In vivo: The tumor growth rate of YK-4-279–treated mice bearing CHP-100 was lower than that in mice having PC3 prostate tumors. The cumulative data from five independent experiments with the ESFT xenografts (TC71 and CHP-100) show a marked overall tumor reduction in the YK-4-279–treated mice. Pathological analysis of mice treated with YK-4-279 did not show any signs of toxicity, except for sterile inflammatory lesions in the abdominal cavities of mice [1].


Clinical trial: No clinical data are available currently.


Reference:
[1] Erkizan HV, Kong Y, Merchant M, Schlottmann S, Barber-Rotenberg JS, Yuan L, Abaan OD, Chou TH, Dakshanamurthy S, Brown ML, Uren A, Toretsky JA.  A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing's sarcoma. Nat Med. 2009;15(7):750-6.