ホームページ Epigenetics Histone Methyltransferase inhibitor - G9a/GLP inhibitor - Anti-infection inhibitor - Thioredoxin Reductase inhibitor Chaetocin For research use only.

Chaetocin

Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR).

Chaetocin化学構造

CAS No. 28097-03-2

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 103500 国内在庫あり
JPY 25000 国内在庫あり
JPY 88000 国内在庫あり
JPY 265500 国内在庫なし(納期7~10日)
JPY 598500 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]
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Chaetocin関連製品

シグナル伝達経路

Histone Methyltransferase Signaling Pathways

Histone Methyltransferaseシグナル伝達経路

Histone Methyltransferase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
Drosophila melanogaster SL2 Function assay 0.1 uM 5 days Inhibition of SU(VAR)3-9 in Drosophila melanogaster SL2 cells assessed as reduction of H3K9me2 at 0.1 uM after 5 days by MALDI-TOF MS seeded at 2.5 million cells/ml density 16408017
Drosophila melanogaster SL2 Function assay 0.5 uM 5 days Inhibition of SU(VAR)3-9 in Drosophila melanogaster SL2 cells assessed as reduction of H3K9me2 at 0.5 uM after 5 days by MALDI-TOF MS seeded at 2.5 million cells/ml density 16408017
HL60 Apoptosis assay 30 uM 4 hrs Induction of apoptosis in human HL60 cells assessed as necrotic cell death at 30 uM after 4 hrs using DAPI/PI by confocal laser microscopy analysis 20675131
HL60 Apoptosis assay 0.3 uM 4 hrs Induction of apoptosis in human HL60 cells assessed as nuclear fragmentation at 0.3 uM after 4 hrs using DAPI/PI by confocal laser microscopy analysis 20675131
HL60 Apoptosis assay 0.3 uM 2 hrs Induction of apoptosis in human HL60 cells assessed as activation of caspase 3 at 0.3 uM after 2 hrs by Western blot analysis 20675131
Drosophila melanogaster SL2 Function assay 0.5 uM Inhibition of SU(VAR)3-9 in Drosophila melanogaster SL2 cells assessed as reduction of H3K9me3 at 0.5 uM by immunostaining method 16408017
Jurkat Cytotoxicity assay 40 hrs Cytotoxicity against human Jurkat cells after 40 hrs bioluminescence assay, IC50 = 0.6 μM. 20303767
Hep3b Function assay Inhibition of HIF-1alpha-mediated VEGF secretion in human Hep3b cells by ELISA, IC50 = 0.1 μM. 22305612
Hep3b Function assay Inhibition of HIF-1alpha-mediated VEGF expression in human Hep3b cells by luciferase reporter gene assay, IC50 = 0.04 μM. 22305612
A549 Cytotoxicity assay Cytotoxicity against human A549 cells, IC50 = 0.025 μM. 20303767
MCF7 Function assay Inhibition of histone-lysine N-methyltransferase in human MCF7 cells assessed as decrease in methylation of RARbeta DNA by qPCR method ChEMBL
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生物活性

製品説明 Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR).
Targets
dSU(VAR)3-9 [1] mouse G9a [1] Neurospora crassa DIM5 [1]
0.8 μM 2.5 μM 3 μM
In Vitro
In vitro

In SL-2 Drosophila tissue culture cells, Chaetocin causes the inhibition of SU(VAR)3-9 and the number of H3 molecules dimethylated at Lys9, and also inhibits cell growth. [1]

In HepG2, Hep3B, and Huh7 human hepatoma cells, Chaetocin inhibits HIF-1-Mediated hypoxic responses. [2]

Chaetocin also potently inhibits proliferation and colony formation in a broad range of cancer cell lines with IC50 of 2-10 nM. [3]
Kinase Assay Methylation assays
Unless otherwise stated, reactions are performed as followed: 1 g of purified enzyme (dSU(VAR)3-9 213; GST-hSUV39H1(82-412); GST-ncDIM5(19-318) and GSTmG9a(621-1000); dPRSET7(1-691); His-SET7/9(109-366) or enzyme complex expressed in a baculoviral expression system (dE(z), dSU(Z)12, dp55, dESC) were incubated for 30 minutes with 1 g of a peptide containing the first 19 amino acids of H3 plus an additional cystein residue (ARTKQTARKSTGGKAPRKQC) in a total volume of 40μl in BC25 (10mM HEPES pH7.6, 25mM NaCl, 1mM EDTA, 10%glycerol). All enzymes except for the E(z) complex had a similar specific activity between 5-10 nmole/min/mg. For the E(z) complex, the specific activity is approximately 5-10 fold lower, which is probably due to an incomplete formation of the full complex that is required for the highest activity. As a methyl donor S-Adenosyl [methyl-3H] methionine (SAM) is present in the reaction at a final concentration of 40 M with a specific activity of 0.3Ci/mmole. Reactions are stopped by adding 1/10 volume of 100% acetic acid and the incorporation of radioactivity is measured by spotting 30 l of the reaction on P81 filter paper and subsequent scintillation counting. For the inhibitor screening, 1 l of inhibitor with a concentration of 10 g/l is added to each reaction. In the cases where PRSET7 or the E(z) complex is used as enzyme either recombinant nucleosomes (1 g) or recombinant H3 (1 g) respectively replaced the H3 peptide as a substrate.
細胞実験 細胞株 HEK293T
濃度 125 nM
反応時間 24 h
実験の流れ

Cells were treated with chaetocin (125 nM) or DMSO for 24 h.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot Procaspase-3 / Cleaved Caspase-3 / PARP 26890137
Growth inhibition assay Cell viability 18176557
In Vivo
In Vivo

In Hepa 1c1c-7 tumor-bearing mice, Chaetocin (0.25 mg/kg, i.p.) inhibits tumor growth by deregulating HIF-1[alpha]-mediated angiogenesis. [2]

In SKOV3 tumor-bearing nude mice, chaetocin treatment (0.25 mg/kg, i.p.) significantly delays the tumor growth with minimal evidence of toxicities. [3]
動物実験 動物モデル Hur7 tumor-bearing mice, Hepa 1c1c-7 tumor-bearing mice
投与量 0.25 mg/kg
投与経路 i.p.

化学情報

分子量 696.84 化学式

C30H28N6O6S4
CAS No. 28097-03-2 SDF Download Chaetocin SDFをダウンロードする
Smiles CN1C(=O)C23CC4(C(N2C(=O)C1(SS3)CO)NC5=CC=CC=C54)C67CC89C(=O)N(C(C(=O)N8C6NC1=CC=CC=C71)(SS9)CO)C
保管

In vitro
Batch:

DMSO : 25 mg/mL ( (35.87 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 : 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

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）

mg/kg g μL 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。

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