YK 4-279是一种RNA解旋酶A 与致癌转录因子EWS-FLI1结合抑制剂，能抑制ESFT细胞增长，诱导凋亡。

YK 4-279, an inhibitor of RNA Helicase A (RHA), binds to the oncogenic transciption factor EWS-FLI1.

在融合阳性LNCaP-luc-M肿瘤小鼠模型中,YK-4-279能够抑制肿瘤细胞的增殖和迁移.在体内ESFT异种移植瘤中,YK-4-279（1.5 mg/kg i.p. ）能够抑制生长.

在含有EWS-FLI1的TC32细胞中,YK-4-279通过阻断EWS-FLI1与RHA的相互作用,减少细胞周期蛋白D的水平。在ESFT细胞中,YK-4-279能够抑制细胞生长,诱导细胞凋亡。在融合阳性前列腺癌细胞中,YK-4-279能够抑制ERG 和 ETV1的生物活性,减少细胞的迁移。

Cytosolic phosphorylation of Akt: Hela cells are serum starved for 1 hr and treated with IGF (100ng/mL) or SC79 (4 μg/mL) for 30 minutes. Cells are lysed in Lysis buffer containing 250 mM Sucrose, 20 mM HEPES, 10 mM KCl, 1.5 mM MgCl2, 1 mM EDTA, 1 mM EGTA supplemented with protease inhibitors. Cells are passed through 25 g needle several times and kept on ice for 20 minutes. Total cell lysate is taken at this point. Cell lysates are centrifuged at 100,000 g for 30 minutes. Supernatant is collected as the cytosolic fraction. Pellet is washed with lysis buffer and represents the membrane fraction. Total cell lysate, cytosolic and membrane fractions are resolved by SDS-PAGE and analyzed for phospho-Akt (S473), Total Akt, Tubulin (cytosolic marker) and Orai1 (membrane marker) by western blotting.

1037184-44-3

C17H13Cl2NO4

366.2

4,7-二氯-1,3-二氢-3-羟基-3-[2-(4-甲氧基苯基)-2-氧代乙基]-2H-吲哚-2-酮

Ethanol:48 mg/mL (131.1 mM)
H2O:<1 mgml
DMSO:68 mg/mL (185.7 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years