YK-4-279

YK-4-279 Basic information
Product Name:YK-4-279
Synonyms:YK-4-279;4,7-Dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indol-2-one;4,7-Dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indol-2-one YK-4-279;YK-4-279;YK 4-279;4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one;CS-1785;2H-Indol-2-one, 4,7-dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-;YK-4-279 USP/EP/BP
CAS:1037184-44-3
MF:C17H13Cl2NO4
MW:366.2
EINECS:
Product Categories:Inhibitors
Mol File:1037184-44-3.mol
YK-4-279 Structure
YK-4-279 Chemical Properties
Melting point 149-151℃
Boiling point 608.9±55.0 °C(Predicted)
density 1.456
storage temp. Store at -20° C.
solubility insoluble in H2O; ≥16.35 mg/mL in DMSO; ≥24.25 mg/mL in EtOH with ultrasonic
form Powder
pka10.43±0.20(Predicted)
Safety Information
MSDS Information
YK-4-279 Usage And Synthesis
Chemical PropertiesA crystalline solid
UsesYK-4-279 is a small molecule inhibitor of EWS-FLI1 protein, and has been shown to disrupt the mitotic progression of neuroblastoma cells, and potentially other cancers.
UsesAn oncogenic fusion protein found in Ewing's sarcoma, a family of undifferentiated tumors which occur throughout the body. The binding of ES-FLI1 to RNA helicase A (RHA) promotes its oncogenic function. Inhibits 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 to 2 μM.1 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.
DefinitionChEBI: 4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one is an aromatic ketone.
Biological Activityyk 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 vitroesft 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 vivothe 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].
storageStore at +4°C
references[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.
YK-4-279 Preparation Products And Raw materials
YL 0919 ZEBULARINE PF-04217903 YKL 06-061 2-(4-HYDROXY-3-METHOXYPHENYL)BENZOTHIAZOLE 6-CHLORO-2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-1-CARBOXAMIDE yk11 YK-3-237 YKL-5-124

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