EGCG ((-)-Epigallocatechin Gallate)

EGCG ((-)-Epigallocatechin Gallate) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.

CAS No. 989-51-5

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
1g	JPY 59500	国内在庫なし(納期7~10日)

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製品安全説明書

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シグナル伝達経路

Telomeraseシグナル伝達経路

Telomerase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
human MDA435/LCC6MDR cells	Function assay	10 μM	5 days	Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversible of paclitaxel resistance measured as IC50 for paclitaxel at 10 uM after 5 days by CellTiter 96 Aqueous assay, IC50=0.1226 μM	25985195
human Caco-2 cells	Growth inhibition assay	25 μM	6 days	Growth inhibition of human Caco-2 cells at 25 uM after 6 days	18324763
mouse 3T3 cells	Function assay	1-20 μM	12 h	Antimigratory activity against Swiss albino mouse 3T3 cells assessed as increase of cell numbers at 1 to 20 uM after 12 hrs by by scratch-wound assay	21080642
human Jurkat cells	Function assay	10-55 μM	24 h	Inhibition of TNFalpha-induced NF-kappaB activation in human Jurkat cells at 10 to 55 uM after 24 hrs by electrophoretic mobility shift assay	21080642
human Raji cells	Growth inhibition assay	10 μM	48 h	Growth inhibition against human Raji cells assessed as cell viability at 10 uM after 48 hrs by trypan blue based microscopic analysis in presence of superoxide dismutase	21434603
human PC3 cells	Proliferation assay	10-100 μM	48 h	Antiproliferative activity against human PC3 cells at 10 to 100 uM after 48 hrs by hemocytometric cell counting method	23867167
human A431 cells	Function assay	100 μM	12 h	Reduction of clustering of GFP-GPI in lipid rafts of human A431 cells at 100 uM after 12 hrs by confocal microscopic analysis	24456004
human SKBR3 cells	Function assay	200μM	30 mins	Downregulation of ErbB2 protein expression in human SKBR3 cells in serum free medium at 200 uM after 30 mins by immunofluorescence staining-based confocal microscopic analysis	24456004
human 293T cells	Function assay	50 μM	12 h	Inhibition of DYRK1A in human 293T cells assessed as reduction of GLI1 transcription activity at 50 uM after 12 hrs by dual-luciferase reporter gene assay	22154664
CHO cells	Cytotoxic assay		48 h	Cytotoxicity against CHO cells expressing OATP1B3 haplotype 1 after 48 hrs by fluorescence based CellTiter-Glo assay, IC50=3.2 μM	23327877
MDCK cells	Function assay		4 days	Antiviral activity against influenza A virus (A/swine/OH/511445/2007(H1N1)) Oh7 infected in MDCK cells assessed as inhibition of viral replication after 4 days by quantitative RT-PCR, ED50=8.3 μM	22115591
human HL60 cells	Proliferation assay		3 days	Antiproliferative activity against human HL60 cells after 3 days, IC50=9.4 μM	18693020
HSC-T6 cells	Function assay		48 h	Antifibrotic activity against rat HSC-T6 cells assessed as inhibition of proliferation after 48 hrs by BrdU incorporation assay, IC50=9.9 μM	21504848
mouse RAW264.7 cells	Function assay		5 days	Inhibition of RANKL-induced osteoclastogenesis in mouse RAW264.7 cells assessed as decrease in TRAP-positive multi-nucleated cells after 5 days, IC50=29.8 μM	21456521
human A431 cells	Proliferation assay		48 h	Antiproliferative activity against human A431 cells overexpressing ErbB in serum-free medium assessed as cell viability after 48 hrs by WST-1 assay, EC50=38 μM	24456004
human MDA-MB-231 cells	Proliferation assay		24 h	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay	22459208
human HepG2 cells	Function assay		24 h	Inhibition of oleic acid-induced triglyceride over-accumulation in human HepG2 cells incubated for 24 hrs relative to untreated control	21824690
human HepG2 cells	Function assay		24 h	Antioxidant activity in human HepG2 cells assessed as reduction of oleic acid-induced ROS generation incubated for 24 hrs by DHCF-DA based fluorimetric assay relative to untreated control	21824690
human MDA-MB-231 cells	Proliferation assay		24 h	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay	22459208
human K562 cells	Function assay		24 h	Induction of 67 kDa laminin receptor expression in human K562 cells after 24 hrs by flow cytometry analysis	21434603
human HL60 cells	Function assay		24 h	Induction of 67 kDa laminin receptor expression in human HL60 cells after 24 hrs by flow cytometry analysis	21434603
SH-SY5Y cells	Function assay			Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release, EC50=0.03987 μM	19138859
Sf9 cells	Function assay			Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintillation counting method, IC50=0.5 μM	25406944
human U937 cells	Function assay			Inhibition of telomerase in human U937 cells, IC50=1 μM	22413845
human HeLa cells	Function assay			Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction followed by compound washout by spin-telomeric repeat amplification protocol, IC50=1.08 μM	22413845
mouse 3T3-L1 cells	Function assay			Inhibition of G6PD-mediated NADPH production in mouse 3T3-L1 cells, IC50=25 μM	18313308
HSC-T6 cells	Proliferation assay			Antiproliferative activity against rat HSC-T6 cells assessed as reduction in cell viability, IC50=29.8 μM	25322455
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生物活性

製品説明

EGCG ((-)-Epigallocatechin Gallate) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.

Targets

telomerase ^[4]

DNMT ^[4]

HER2 ^[5]

EGFR ^[5]

FASN ^[6]

In Vitro
In vitro	(-)-Epigallocatechin gallate functions as a powerful antioxidant, preventing oxidative damage in healthy cells, but also as an antiangiogenic and antitumor agent and as a modulator of tumor cell response to chemotherapy. (-)-Epigallocatechin gallate shows multiple anticancer effects, such as anti-proliferation, anti-angiogenesis, transformation prevention of various cancer cells, cancer cell cycle arrest and inhibition of tumor metastasis. (-)-Epigallocatechin gallate exerts multi-anticancer effects through regulating several cancer-related cell signal pathways (regulated the function or the expression of key signal proteins, such as nuclear factor-κB, MAPKs and activator protein-1, EGFR, IGF, COX-2 signaling pathway, and so on.), effecting methylation of cancer genes and combination of ligand with membrane receptors. ^[1] (-)-Epigallocatechin gallate also shows an immunomodulating effects. Several types of immune cells in both the innate and adaptive immune systems are known to be affected in varying degrees by (-)-Epigallocatechin gallate. Among them, the dramatic effect on T cell functions has been repeatedly demonstrated, including T cell activation, proliferation, differentiation, and production of cytokines. Studies using animal models of autoimmune diseases have reported disease improvement in animals treated with green tea/EGCG. ^[2] (-)-Epigallocatechin gallate displays anti-infective properties. Antiviral activities of (-)-Epigallocatechin gallate with different modes of action have been demonstrated on diverse families of viruses, such as Retroviridae, Orthomyxoviridae and Flaviviridae and include important human pathogens like human immunodeficiency virus, influenza A virus and the hepatitis C virus. ^[3]
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	β-catenin / p-AKT / Cyclin D1 p-MAPK / MAPK Notch1 / Notch2		28693189
	Growth inhibiton assay	Cell proliferation Cell viability		23525843

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05758571	Recruiting	Interstitial Pneumonia\|Neoplasms Malignant	Shandong Cancer Hospital and Institute	January 5 2023	Phase 1\|Phase 2
NCT03928847	Completed	Idiopathic Pulmonary Fibrosis	Hal Chapman\|National Heart Lung and Blood Institute (NHLBI)\|University of California San Francisco	December 1 2017	Early Phase 1

参考
[1] Khan N, et al. Cancer Res, 2006, 66(5), 2500-2505. [2] Pae M, et al. Food Funct, 2013, 4(9), 1287-1303. [3] Steinmann J, et al. Br J Pharmacol. 2013 Mar;168(5):1059-1073. [4] Brahma N Singh, et al. Biochem Pharmacol . 2011 Dec 15;82(12):1807-21. [5] Martiniano Bello, et al. Int J Biol Macromol . 2018 May;111:569-586. [6] Ariadna Giró-Perafita, et al. Clin Cancer Res . 2016 Sep 15;22(18):4687-97. + 展開

参考

+ 展開

化学情報

分子量	458.37	化学式	C₂₂H₁₈O₁₁
CAS No.	989-51-5	SDF	Download EGCG ((-)-Epigallocatechin Gallate) 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 : 91 mg/mL ( (198.52 mM)； Warmed with 50℃ water bath; 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 : 91 mg/mL

Ethanol : 91 mg/mL

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):