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Butein

CAS No. : 487-52-5

MCE 站：Butein

产品活性：Butein 是一种 cAMP 特异性的 PDE 抑制剂，对 PDE4 的 IC₅₀为 10.4 μM。Butein 是蛋白酪氨酸激酶抑制剂，对 EGFR 和 p60^c-src 的 IC₅₀ 分别为 16 和 65 μM。Butein 通过 AKT 和 ERK/p38 MAPK 通路，靶向 FoxO3a 使 HeLa 细胞对 Cisplatin 敏感。Butein 还是一种 SIRT1 激活剂 (STAC)。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK  |  Autophagy  |  Apoptosis  |  Metabolic Enzyme/Protease

作用靶点：EGFR  |  Autophagy  |  Apoptosis  |  Phosphodiesterase (PDE)

In Vitro: Butein potently inhibits cAMP-specific phosphodiesterase (type IV) activity with an IC₅₀ of 10.4±0.4 μM. In contrast, phosphodiesterase I, III and V activities were inhibited by Butein above 100 μM.
Butein, a plant polyphenol, is a specific protein tyrosine kinase inhibitor. Butein inhibits not only the EGF-stimulated auto-phosphotyrosine level of EGFR in HepG2 cells but also tyrosine-specific protein kinase activities of EGFR (IC₅₀=16 μM) and p60^c-src (IC₅₀=65 μM) in vitro.
Butein (10, 20, and 40 μM; 24, 48, and 72 hours) inhibits cell growth in a dose- and time-dependent manner.
Butein exhibits anticancer activity through the inhibition of the activation of PKB/AKT and MAPK pathways, which are two pathways known to be involved in resistance to cisplatin. Butein (20 ?M) decreases phosphorylation of AKT, ERK and p38 following 24 h of co-treatment with Cisplatin (20 ?M).

In Vivo: Butein (2 mg/kg every 2 days) in combination with Cisplatin (2 mg/kg every 2 days) for 3 weeks suppresses tumor growth in vivo.

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