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YK-4-279
Cat No.
CEI-1589
Description
YK-4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1
Product Overview
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.
CAS No.
1037184-44-3
Molecular Weight
366.2
Purity
0.98
Storage
Store at -20°C
Synonyms
YK 4-279
Targets
RHA
Molecular Formula
C17H13Cl2NO4
Chemical Name
4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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.
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.
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