YK 4-279

Based on 18 reference(s) in Google Scholar 9 10 18

Axon 2469

CAS [1037184-44-3]

MF C17H13Cl2NO4
MW 366.20

Purity: 99%
Soluble in DMSO

YK 4-279

Description

Inhibitor of interactions between the fusion protein EWS-FLI1 and RNA helicase A (RHA; Kd value 9.48 µM) with a detrimental effect on ESFT cells both in vitro and in vivo. YK-4-279 is also found to potently inhibit biological activity of ERG (Kd value 11.7 µM) and ETV1 (Kd value 17.4 µM) resulting in suppression of both primary tumor growth and metastasis of fusion positive prostate cancer xenografts. ETV1 is a member of the translocated erythroblastosis virus E26 transforming sequence (ETS) family of transcription factors) and targets MMP7, MMP13, FKBP10 and GLYATL2 genes, among several others.

S. Rahim et al. A small molecule inhibitor of ETV1, YK-4-279, prevents prostate cancer growth and metastasis in a mouse xenograft model. PLoS One. 2014 Dec 5;9(12):e114260.

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

H.V. Erkizan 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.

Apoptosis Cell Signaling & Oncology Oncogene Fusion Proteins Transcription Factors Helicase-Primase ETV1 ERG TF class 3.5.2.2.4 Antiviral agents Infectious Disease

Inhibitor of ETV1, ERG and interactions of EWS-FLI1 and RNA helicase A

Chemical name

4,7-dichloro-3-hydroxy-3-(2-(4-methoxyphenyl)-2-oxoethyl)indolin-2-one

Parent CAS No.

[1037184-44-3]

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YK 4-279

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