同義詞：   4',5,7-Trihydroxyflavone  

應(yīng)用；   An antiinflammatory casein kinase II inhibitor  

CAS號(hào)碼:   520-36-5  

純度:   ≥98%  

分子量:   270.24  

分子式:   C₁₅H₁₀O₅  

* 參考分析證明 大量特定數(shù)據(jù) (包括水 含量).

介紹 技術(shù)信息 安全信息 安全技術(shù)說明書和分析證明書

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.

參考文獻(xiàn)

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

外觀 :

Powder

物理狀態(tài) :

Solid

溶解度 :

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

保存 :

Store at -20° C

熔點(diǎn) :

>300° C (lit.)

沸點(diǎn) :

~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 數(shù)據(jù) :

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)

僅供科研使用。不可用于診斷或治療。  

德國水公害等級(jí) :

3

RTECS :

LK9276000

PubChem CID :

5280443

默克索引 :

14: 730

MDL 號(hào)碼 :

MFCD00006831

EC號(hào)碼 :

208-292-3

Beilstein 注冊(cè) :

262620

SMILES :

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