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K-80003

CAS No. : 1292821-90-9

MCE 国际站：K-80003

产品活性：K-80003 有效抑制 tRXRα 依赖性的 Akt 激活和肿瘤细胞生长。

研究领域：PI3K/Akt/mTOR

作用靶点：Akt

In Vitro: When MCF-7 cells are cotreated with K-80003, TNFα-induced colocalization of tRXRα with p85α in the cytoplasm is inhibited, resulting in tRXRα nuclear localization. Western blotting shows that K-80003-stabilized tetrameric form of tRXRα is found exclusively in the nuclear fraction, while tRXRα monomer is distributed both in the nuclear and cytoplasmic fractions.

In Vivo: K-80003 is a potent inhibitor of AKT activation by all-trans-retinoic acid. K-80003 displays enhanced efficacy in inhibiting tRXRα-dependent AKT activation and tRXRα tumor growth in animals. K-80003 has high affinity to RXRα but lacks COX inhibitory activity.

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