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Butein

CAS No. : 487-52-5

MCE 国际站：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 µM) decreases phosphorylation of AKT, ERK and p38 following 24 h of co-treatment with Cisplatin (20 µM).

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.

相关产品：Natural Product Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Metabolism/Protease Compound Library | Protein Tyrosine Kinase Compound Library | Natural Product Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Phenols Library | Traditional Chinese Medicine Monomer Library | Anti-Alzheimer’s Disease Compound Library | Anti-Hepatitis C Virus Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | MG-132 | LY294002 | Doxorubicin hydrochloride | Bafilomycin A1 | Paclitaxel | Y-27632 dihydrochloride | Acetylcysteine | Angiotensin II human | SP600125 | 5-Fluorouracil | Staurosporine | Bortezomib | Tamoxifen | 2-Deoxy-D-glucose | Gemcitabine | Verteporfin | Decitabine | Actinomycin D | Temozolomide | Gefitinib | BAY 11⁻⁷082 | Etoposide | Mitomycin C | CCCP | DAPT | Rotenone | Trastuzumab | Etomoxir | IBMX

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