产品描述: YK-4-279 blocks RNA Helicase A (RHA) binding with EWS-FLI1 (oncogenic protein). YK-4-279 induces apoptosis and shows anti-proliferation activities towards various cancer cells. YK-4-279 has a chiral center and it can be separated into two enantiomers. YK-4-279 can be used for the research of cancer |
靶点:
IC50: 0.94 µM (TC32), 1.83 µM (TC71), 1.03 µM (RDES), 0.33 µM (SKES), 0.94 µM (MMH-ES-1), 0.60 µM (STA-ET 7.2), 1.46 µM (A4573), 4.95 µM (PC3), 22.82 µM ( MCF7), 0.82 µM (MDA-MB-231), 1.514 µM (PANC1), 14.28 µM (ASPC1);Apoptosis;DNA/RNASynthesis |
体内研究:
YK-4-279 (1.5 mg; i.p. once) inhibited ESFT tumor growth |
参考文献:
1. 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. 2. 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. |
溶解性:
DMSO : 25 mg/mL (68.27 mM; Need ultrasonic) |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.731 ml |
13.654 ml |
27.307 ml |
5 mM |
0.546 ml |
2.731 ml |
5.461 ml |
10 mM |
0.273 ml |
1.365 ml |
2.731 ml |
50 mM |
0.055 ml |
0.273 ml |
0.546 ml |
|
注意: |
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