1. Epigenetics
    Anti-infection
  2. Histone Methyltransferase
    Bacterial
    Antibiotic
  3. Chaetocin

Chaetocin 

製品番号: HY-N2019 純度: 98.18%
取扱説明書

Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC50 of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM.

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Chaetocin 構造式

Chaetocin 構造式

CAS 番号 : 28097-03-2

容量 価格(税別) 在庫状況 数量
10 mM * 1  mL in DMSO USD 828 在庫あり
Estimated Time of Arrival: December 31
1 mg USD 180 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 540 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 972 在庫あり
Estimated Time of Arrival: December 31
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100 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC50 of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM.

IC50 & Target

IC50: 0.6 μM (HMT)[1], 4 μM (TrxR)[2]

体外実験

Chaetocin is initially isolated from the fermentation broth of chaetomium minutum and belongs to the class of 3-6 epidithio-diketopiperazines (ETPs). The IC50 for SU(VAR)3-9 is 0.6 μM and acts as a competitive inhibitor for S-adenosylmethionine. Chaetocin inhibits the human ortholog of dSU(VAR)3-9 with a similar IC50 value of 0.8 μM. It inhibits other known Lys9-specific HMTs such as mouse G9a and Neurospora crassa DIM5 with a higher IC50 values of 2.5 and 3 mM, respectively[1]. Chaetocin inhibits TrxR1-initiated turnover of the synthetic substrate DTNB in a cell-free assay in a dose-responsive manner with an IC50 of about 4 μM[2].

体内実験

SL-2 Drosophila tissue cells are cultured in the presence or absence of the inhibitor. Chaetocin has a toxic effect on cells grown in culture. Toxicity is highly dependent on the initial cell density when chaetocin is added to the culture. The number of H3 molecules dimethylated at Lys9 (H3K9me2) is markedly reduced when cells are grown in medium containing 0.5 μM chaetocin after 5 d. Histones isolated from cells treated with 0.1 μM and for a shorter time also shows a drop in Lys9 methylation, but not as strongly as with the higher concentration[1].

分子量

696.84

分子式

C₃₀H₂₈N₆O₆S₄

CAS 番号

28097-03-2

SMILES

O=C([[email protected]@](N1C)(SS2)CO)N3[[email protected]](NC4=CC=CC=C54)([H])[[email protected]]5([[email protected]@]6(C7=CC=CC=C7N8)[[email protected]@]8([H])N(C9=O)[[email protected]](C%10=O)(SS[[email protected]]9(CO)N%10C)C6)C[[email protected]]32C1=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 26 mg/mL (37.31 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4350 mL 7.1752 mL 14.3505 mL
5 mM 0.2870 mL 1.4350 mL 2.8701 mL
10 mM 0.1435 mL 0.7175 mL 1.4350 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.98 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.98 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
細胞実験
[2]

HeLa cells are transfected with 1 μg pcDNA or pcDNA-Trx. Twenty four h after transfection the cells are treated with either DMSO, 100 nM chaetocin or 100 nM doxorubicin for 24 h. The cells are then trypsinized and manually counted in trypan blue to exclude dead cells. For immunoblotting (24 h after transfections), cells are trypsinized, ished in cold PBS, and lysed in CelLytic lysis buffer containing protease inhibitors. Protein is analyzed by BCA assay and lysates are electrophoresed on 15% SDS-PAGE gels and transferred to nitrocellulose. Immunoblotting for thioredoxin and actin is then performed[2].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

純度: 98.18%

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Keywords:

ChaetocinHistone MethyltransferaseBacterialAntibioticInhibitorinhibitorinhibit

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製品名:
Chaetocin
製品番号:
HY-N2019
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