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

Chaetocin  (Synonyms: ケトシン)

製品番号: HY-N2019 純度: 99.22%
COA 取扱説明書 Technical Support

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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CAS 番号 : 28097-03-2

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 751 在庫あり
Solution
10 mM * 1 mL in DMSO USD 751 在庫あり
Solid
1 mg $160 在庫あり
5 mg $490 在庫あり
10 mg $855 在庫あり
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カスタマーレビュー

Based on 10 publication(s) in Google Scholar

Chaetocin 関連抗体

Top Publications Citing Use of Products

    Chaetocin purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 Oct 27:102424.  [Abstract]

    Inhibiting H3K9me3 increased the expression of ribosome-related genes. Human CCs were treated with the H3K9me3 inhibitor Chaetocin (50 nM; 24 h), and RT‒qPCR was performed to measure the expression levels of ribosome-related genes.

    Chaetocin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 May 21;15(1):4327.  [Abstract]

    Flow cytometry analysis of PD-1, SLAMF6, CD44, and CD62L expression in CD8+ T cells activated and expanded in vitro for 5 days with the treatment of Chaetocin (2-10 nM).

    Chaetocin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 May 21;15(1):4327.  [Abstract]

    The potency of Chaetocin (5 nM) amplifyed the antitumor efficacy of OT1 cells in C57BL/6 mice bearing B16-OVA tumors.

    Chaetocin purchased from MedChemExpress. Usage Cited in: Biomaterials. 2024 Jul 27:312:122715.  [Abstract]

    Chaetocin (5 nM; 7 d), a H3K9me3 inhibitor, decreased the CCP in MSCs on stiff ECM.

    Chaetocin purchased from MedChemExpress. Usage Cited in: Clin Transl Med. 06 May 2022.

    Chaetocin (0.01-1 μM; 48 h) efficiently inhibited the proliferation of various lung cancer cell lines tested in a dose-dependent manner, and the IC50 values of Chaetocin against H460, H661, and A549 cells were as low as 61, 68, and 0.11 μM, respectively.

    Histone Methyltransferase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

    Antibiotic アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

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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]
    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    < 0.025 3
    Compound: 12
    Cytotoxicity against human A549 cells
    Cytotoxicity against human A549 cells
    		[PMID: 20303767]
    A549 IC50
    <0.025 3
    Compound: 12
    Cytotoxicity against human A549 cells
    Cytotoxicity against human A549 cells
    		[PMID: 20303767]
    Hep 3B2 IC50
    0.1 3
    Compound: 4
    Downregulation of VEGF protein level in human Hep3B cells after 8 hrs by ELISA
    Downregulation of VEGF protein level in human Hep3B cells after 8 hrs by ELISA
    		[PMID: 30682255]
    Jurkat IC50
    <0.6 3
    Compound: 12
    Cytotoxicity against human Jurkat cells after 40 hrs bioluminescence assay
    Cytotoxicity against human Jurkat cells after 40 hrs bioluminescence assay
    		[PMID: 20303767]
    HL-60 IC50
    0.127 1
    Compound: Chemical Probe: Chaetocin
    Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay
    		[PMID: 25978433]
    HL-60 IC50
    0.153 1
    Compound: Chemical Probe: Chaetocin
    Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay
    		[PMID: 25978433]
    Hep 3B2 IC50
    0.1 3
    Compound: 4
    Downregulation of VEGF protein level in human Hep3B cells after 8 hrs by ELISA
    Downregulation of VEGF protein level in human Hep3B cells after 8 hrs by ELISA
    		[PMID: 30682255]
    Jurkat IC50
    < 0.6 3
    Compound: 12
    Cytotoxicity against human Jurkat cells after 40 hrs bioluminescence assay
    Cytotoxicity against human Jurkat cells after 40 hrs bioluminescence assay
    		[PMID: 20303767]
    KG-1a IC50
    0.095 1
    Compound: Chemical Probe: Chaetocin
    Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 48 hrs by MTT assay
    		[PMID: 25978433]
    KG-1a IC50
    0.103 1
    Compound: Chemical Probe: Chaetocin
    Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 24 hrs by MTT assay
    		[PMID: 25978433]
    U-937 IC50
    0.082 1
    Compound: Chemical Probe: Chaetocin
    Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay
    		[PMID: 25978433]
    U-937 IC50
    0.096 1
    Compound: Chemical Probe: Chaetocin
    Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay
    		[PMID: 25978433]
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Chaetocin 関連抗体
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    696.84

    分子式

    C30H28N6O6S4
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

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

    Chaetomium species
    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 : 12.5 mg/mL (17.94 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体積 （開始）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: 2.08 mg/mL (2.98 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.58%

    COA (256 KB) HNMR (271 KB) RP-HPLC (252 KB)

    取扱説明書 (2659 KB)
    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].

    MedChemExpress (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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.4350 mL 7.1752 mL 14.3505 mL 35.8762 mL
    5 mM 0.2870 mL 1.4350 mL 2.8701 mL 7.1752 mL
    10 mM 0.1435 mL 0.7175 mL 1.4350 mL 3.5876 mL
    15 mM 0.0957 mL 0.4783 mL 0.9567 mL 2.3917 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
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    Chaetocin Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Chaetocin28097-03-2Histone MethyltransferaseBacterialAntibioticInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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