Apigenin

Apigenin is a potent P450 inhibitor for CYP2C9 with K_i of 2 μM.

CAS No. 520-36-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
50mg	JPY 22000	国内在庫あり
100mg	JPY 34000	国内在庫あり
1g	JPY 103500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（29）

カスタマーフィードバック4个实验数据

製品安全説明書

現在のバッチを見る：純度： 99.73%

99.73

Apigenin関連製品

関連ターゲット	P450 CYP2 CYP51 CYP3 CYP735 CYP11 CYP26 CYP2C9 CYP1 CYP17	もっと見る
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シグナル伝達経路

P450 (e.g. CYP17)シグナル伝達経路

P450 (e.g. CYP17)阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
human THP1 cells	Function assay	20 uM	1 h	Inhibition of NOX2 in human THP1 cells assessed as downregulation of TPA-induced CD36 mRNA expression at 20 uM incubated for 1 hr prior to TPA challenge measured after 24 hrs by RT-PCR analysis	23786520
MDA-MB-231 cells	Function assay	5 uM		Inhibition of PMA-stimulated NF-kappaB signaling (unknown origin) expressed in MDA-MB-231 cells at 5 uM incubated for 16 hrs by luciferase reporter gene assay	25190466
human MV4-11 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=2.81 μM	23411073
mouse RAW264.7 cells	Function assay		24 h	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs by Griess reagent method, IC50=6.7 μM	19778086
human H9 cells	Function assay		3 days	Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay, EC50=9 μM	8158164
HEK293 cells	Function assay		24 h	Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=24.9 μM	24955889
mouse 26-L5 cells	Proliferation assay		72 h	Antiproliferative activity against mouse 26-L5 cells after 72 hrs by MTT assay, EC50=25 μM	12027739
human RS4:11 cells	Cytotoxicity assay		72 h	Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=27.9 μM	23411073
mouse B16-BL6 cells	Proliferation assay		72 h	Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay, EC50=31.6 μM	12027739
human H9 cells	Cytotoxicity assay		3 days	Cytotoxicity against human H9 cells after 3 days, IC50=35 μM	8158164
human HT1080 cells	Proliferation assay		72 h	Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay, IC	12027739
mouse L929 cells	Function assay		15 mins	Potentiation of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by crystal violet staining	9287415
mouse RAW264.7 cells	Function assay			Inhibition of COX2 protein expression in mouse RAW264.7 cells, IC50=0.5 μM	16038536
human H295R cells	Function assay			Inhibition of aromatase expressed in human H295R cells, IC50=1 μM	18778944
HEK293 FS cells	Function assay			Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=1.13 μM	20731357
human HeLa cells	Function assay			Inhibition of MRP1 transfected in human HeLa cells assessed as inhibition of [3H]LTC4 transport by rapid filtration assay, Ki=2.4 μM	19725578
human mast cells	Function assay			Inhibition of SYK in human mast cells assessed as reduction in mast cell degranulation, EC50=3 μM	21354800
MDCK cells	Function assay			Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=3.1 μM	21354800
human MDA-kb2 cells	Function assay			Antagonist activity at androgen receptor in human MDA-kb2 cells assessed as inhibition of DHT-induced luciferase activity by luciferase reporter gene assay, IC50=5.2 μM	19592245
MCF-7 MX cells	Function assay			Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=5.9 μM	21354800
MDCK cells	Cytotoxicity assay			Cytotoxicity against MDCK cells by MTT assay, CC50=39.59 μM	18640042
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生物活性

製品説明

Apigenin is a potent P450 inhibitor for CYP2C9 with K_i of 2 μM.

特性

Much more potent than kaempferol and myricetin in CT-L inhibition.

Targets

CYP2C9 ^[5]

2 μM(Ki)

In Vitro
In vitro	Apigenin inhibits PKC by competing with adenosine triphosphate (ATP). Apigenin also reduces the level of TPA-stimulated phosphorylation of cellular proteins and inhibits TPA-induced c-jun and c-fos expression. Apigenin exhibits the reverting effect on the transformed morphology of v-H-ras transformed NIH3T3 cells. ^[1] Apigenin has been shown to possess anti-mutagenic properties in a setting of nitropyrene-induced genotoxicity in Chinese hamster ovary cells. Apigenin suppresses of LPS-induced cyclooxygenase-2 and nitric oxide synthase-2 activity and expression in mouse macrophages. Apigenin has been reported to inhibit protein kinase C activity, mitogen-activated protein kinase (MAPK), transformation of C3HI mouse embryonic fibroblasts and downstream oncogenes in v-Ha-ras-transformed NIH3T3 cells. Apigenin blocks peroxisome proliferation-regulated kinase (ERK), a MAPK in isolated hepatocytes. Apigenin has further been shown to down-regulate the expression of the Na⁺/Ca²⁺-exchanger, a protein important for calcium extrusion in neonatal rat cardiac myocytes. Apigenin induces a reversible G2/M and G0/G1 arrest by inhibiting p34 (cdc2) kinase activity, accompanied by increased p53 protein stability in epidermal cells and fibroblasts. Apigenin is also effective in inhibiting TNFα-induced intracellular adhesion molecule-1 upregulation in cultured human endothelial cells. Apigenin inhibits the expression of HIF-1α and VEGF via the PI3K/Akt/p70S6K1 and HDM2/p53 pathways in human ovarian cancer cells. ^[2] Apigenin inhibits differentiation by suppressing MAPK signal transduction and reducing API transcription factor level in human keratinocytes. Apigenin also inhibits proliferating of human keratinocytes. ^[3]
細胞実験	細胞株	WI-38, T-24, HT-1376 and PC-3 cells
	濃度	0, 1, 5, 10, 20, 30, 40, and 50 μg/ml
	反応時間	24 h
	実験の流れ	To measure the effect of apigenin on cell viability, the WI-38, T-24, HT-1376 and PC-3 cells were seeded in 24-well plates (1 × 10⁵ cells/well) for 16-18 h. The cells were then treated with or without various concentrations (0, 1, 5, 10, 20, 30, 40, and 50 μg/ml) of apigenin for 24 h. Each treatment was repeated 3 times. After the exposure period, the medium was removed and followed by washing the cells with PBS. The medium was then changed and incubated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution (5 mg/ml)/well for 4 h. The medium was removed, and formazan was solubilised in isopropanol and measured spectrophotometrically at 563 nm. The percentage of viable cells was estimated by comparing them with the untreated control cells.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	MHC / MHC2A / MHC2B / MyoD CXCR4 CDK1 / Cyclin B1 / p21		29108230
	Immunofluorescence	E-caherin / Vimentin Snail		27203387
	Growth inhibition assay	Cell viability		23224239

In Vivo
In Vivo	Apigenin down-regulates production of IL-4 in ovalbumin-immunized BALB/C mice. Apigenin inhibits melanoma lung metastases by impairing interaction of tumor cells with endothelium. Apigenin is shown to cause a significant increase in uterine weight and overall uterine concentration of estrogen receptor (ER)-α in female mice (64) and also suppresses prostate and breast cancer cell growth through estrogen receptor β1. Apigenin suppresses the levels of IGF-I in prostate tumor xenografts and increases levels of IGFBP-3, a binding protein that sequesters IGF-I in vascular circulation. ^[2] Apigenin (12.5 mg/kg) increases cell proliferation in the dentate gyrus of hippocampus of adult mice. ^[4]
動物実験	動物モデル	heterozygous C57BL/TGN TRAMP mice
	投与量	20 and 50 μg/mouse/day
	投与経路	p.o.

参考
[1] Lin JK, et al. J Cell Biochem Suppl, 1997, 28-29, 39-48. [2] Shukla S, et al. Pharm Res, 2010, 27(6), 962-978. [3] Balasubramanian S, et al. Toxicol Appl Pharmacol, 2007, 224(3), 214-219. [4] Taupin P, et al. Expert Opin Ther Pat, 2009, 19(4), 523-527. [5] Shi MD, et al. Cancer Cell Int. 2015, 15:33. [6] Shukla S, et al. Carcinogenesis. 2014, 35(2):452-60. + 展開

参考

+ 展開

化学情報

分子量	270.24	化学式	C₁₅H₁₀O₅
CAS No.	520-36-5	SDF	Download Apigenin SDFをダウンロードする
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 54 mg/mL ( (199.82 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):