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| | 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 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 | | pka | 10.43±0.20(Predicted) |
| | YK-4-279 Usage And Synthesis |
| Chemical Properties | A crystalline solid | | Uses | An 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. | | Uses | YK-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. | | Definition | ChEBI: 4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one is an aromatic ketone. | | Biological Activity | 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]. | | storage | Store 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 |
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