YK-4-279

Modify Date: 2024-01-02 16:39:40

YK-4-279 Structure
YK-4-279 structure
Common Name YK-4-279
CAS Number 1037184-44-3 Molecular Weight 366.195
Density 1.5±0.1 g/cm3 Boiling Point 608.9±55.0 °C at 760 mmHg
Molecular Formula C17H13Cl2NO4 Melting Point 149-151℃
MSDS N/A Flash Point 322.1±31.5 °C

 Use of YK-4-279


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.

 Names

Name 4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one
Synonym More Synonyms

 YK-4-279 Biological Activity

Description 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.
Related Catalog
References

[1]. 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.

[2]. Rahim S, et al. YK-4-279 inhibits ERG and ETV1 mediated prostate cancer cell invasion. PLoS One. 2011 Apr 29;6(4):e19343.

[3]. 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.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 608.9±55.0 °C at 760 mmHg
Melting Point 149-151℃
Molecular Formula C17H13Cl2NO4
Molecular Weight 366.195
Flash Point 322.1±31.5 °C
Exact Mass 365.022156
PSA 75.63000
LogP 3.03
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.631
Storage condition Store at -20° C.

 Safety Information

Hazard Codes Xi

 Synonyms

4,7-Dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1,3-dihydro-2H-indol-2-one
cs-0667
yk4-279
2H-Indol-2-one, 4,7-dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-
YK-4-279
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