同义词：   4',5,7-Trihydroxyflavone  

应用；   An antiinflammatory casein kinase II inhibitor  

CAS号码:   520-36-5  

纯度:   ≥98%  

分子量:   270.24  

分子式:   C₁₅H₁₀O₅  

* 参考分析证明 大量特定数据 (包括水 含量).

介绍 技术信息 安全信息 安全技术说明书和分析证明书

Apigenin is an antioxidant plant flavonoid which contains antiinflammatory and anticancer properties. It may induce apoptosis and inhibit proliferation of tumor cells by arresting the cell cycle at the G₂/M phase. Apigenin is also known to be a MAP kinase inhibitor and a selective inhibitor of casein kinase II (CK2). Apigenin is capable of exerting diverse effects on a vast variety of molecular targets. Most effects appear to be mediated via the suppression of nitric oxide synthase-2 (NOS2), Hypoxia-inducible factor 1 α (HIF-1α), lipoxygenase, cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF) expression. Apigenin blocks proliferation of Wnt-1 transfected cells, dephosphorylates β-catenin and lowers levels of β-catenin and Dvi. Additionally, apigenin is an inhibitor of CYP19, CYP2C9, and ERK.

参考文献

1. Shen, J., et al. J. 2001. Immunol. 167: 4919-4925. PMID: 1167349
2. Song D.H., et al. 2000. J. Biol. Chem. 275: 23790-23797. PMID: 10806215
3. Yamada, M., et al. 2005. Proc. Natl. Acad. Sci. U.S.A. 102: 7736-7741. PMID: 15897466
4. Ujiki, M.B., et al. 2006. Molecular Cancer. 5: 76. PMID: 17196098
5. Fang, J., et al. 2006. Carcinogenesis. 28: 858-864. PMID: 17071632
6. Shukla, S., et al. 2006. Mol Cancer Ther. 5: 843-852. PMID: 16648554
7. Liang YC., et al. 1999. Carcinogenesis. 20: 1945-1952. PMID: 10506109
8. Fang, J., et al. 2005. FASEB J. 19: 342-353. PMID: 15746177

外观 :

Powder

物理状态 :

Solid

溶解度 :

Soluble in DMSO (27 mg/mL) or 1M KOH (50mg/ml)

保存 :

Store at -20° C

熔点 :

>300° C (lit.)

沸点 :

~555.51° C at 760 mmHg (Predicted)

密度 :

~1.5 g/cm    ³ (Predicted)

折射率 :

n    ²⁰    _D 1.73

IC50 :

TPA: IC    ₅₀ = 59.44 M (human breast cancer cells); TPA: IC    ₅₀ = 31.15 M (human breast cancer cells); ATP: IC    ₅₀ = 10 ± 0.5 M (protein kinase C); yrosine kinases fibroblast growth factor receptor: IC    ₅₀ = 20 M (protein kinase C); pp60v-src: IC    ₅₀ = >200 M (protein kinase C)

Ki 数据 :

Adenosine A2a receptor: K    _i= 7580 nM (Rattus norvegicus); Butyrylcholinesterase: K    _i= 37400 nM (Homo sapiens); Cytochrome P450 1A1: K    _i= 390 nM (Homo sapiens); Cytochrome P450 1B1: K    _i= 64 nM (Homo ); Casein kinase II alpha: K    _i= 740 nM (Homo ); Multidrug resistance-associated protein 1: K    _i= 2400 nM (Homo ); GABA-A receptor; anion channel: K    _i= 770 nM (Rattus norvegicus); Adenosine A1 receptor: K    _i= 3000 nM (Rattus norvegicus); Acetylcholinesterase: K    _i= 12160 nM (Homo sapiens)

仅供科研使用。不可用于诊断或治疗。  

德国水公害等级 :

3

RTECS :

LK9276000

PubChem CID :

5280443

默克索引 :

14: 730

MDL 号码 :

MFCD00006831

EC号码 :

208-292-3

Beilstein 注册 :

262620

SMILES :

C1=CC(=CC=C1C2=CC(=O)C3=C(C=C(C=C3O2)O)O)O