Chaetocin
Based on 10 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.22%
- CAS No.: 28097-03-2
- Formula: C30H28N6O6S4
- Molecular Weight:696.84
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Chaetocin
More- Nat Commun. 2024 May 21;15(1):4327. [Abstract]
- Autophagy. 2025 Nov 23:1-13. [Abstract]
- Adv Sci (Weinh). 2025 Oct 20:e07908. [Abstract]
- Biomaterials. 2024 Jul 27:312:122715. [Abstract]
- Cell Rep Med. 2025 Oct 27:102424. [Abstract]
- Clin Transl Med. 06 May 2022.
- Cell Mol Life Sci. 2024 Jul 8;81(1):292. [Abstract]
- Biochem J. 2023 Mar 31;480(6):421-432. [Abstract]
- Breast Cancer. 2022 Sep;29(5):854-868. [Abstract]
- Research Square Print. September 20th, 2022.
Customer Validation & Images
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RT-PCR
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Flow Cytometry
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In Vivo Efficacy Study
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
All Histone Methyltransferase Isoforms
MoreAll Antibiotic Isoforms
More
Biological Activity
IC50: 0.6 μM (HMT)[1], 4 μM (TrxR)[2]
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
<0.025 μM
Compound: 12
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Cytotoxicity against human A549 cells
Cytotoxicity against human A549 cells
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[PMID: 20303767] |
| Hep 3B2 | IC50 |
0.1 μM
Compound: 4
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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
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[PMID: 30682255] |
| HL-60 | IC50 |
0.127 nM
Compound: Chemical Probe: Chaetocin
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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
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[PMID: 25978433] |
| HL-60 | IC50 |
0.153 nM
Compound: Chemical Probe: Chaetocin
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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
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[PMID: 25978433] |
| Jurkat | IC50 |
<0.6 μM
Compound: 12
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Cytotoxicity against human Jurkat cells after 40 hrs bioluminescence assay
Cytotoxicity against human Jurkat cells after 40 hrs bioluminescence assay
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[PMID: 20303767] |
| KG-1a | IC50 |
0.095 nM
Compound: Chemical Probe: Chaetocin
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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
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[PMID: 25978433] |
| KG-1a | IC50 |
0.103 nM
Compound: Chemical Probe: Chaetocin
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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
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[PMID: 25978433] |
| U-937 | IC50 |
0.082 nM
Compound: Chemical Probe: Chaetocin
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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
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[PMID: 25978433] |
| U-937 | IC50 |
0.096 nM
Compound: Chemical Probe: Chaetocin
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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
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[PMID: 25978433] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 28097-03-2
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Appearance Solid
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Molecular Weight 696.84
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Formula C30H28N6O6S4
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Color White to yellow
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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
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Structure Classification
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Initial Source
Chaetomium species
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Nat Commun
Priming with LSD1 inhibitors promotes the persistence and antitumor effect of adoptively transferred T cells. [Abstract]2024 May 21;15(1):4327. PMID: 38773088
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.
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Autophagy
Autophagy regulates the maternal-to-zygotic transition through MAP1LC3B-mediated maternal mRNA decay. [Abstract]2025 Nov 23:1-13. PMID: 41231099 -
Adv Sci (Weinh)
Morphine Tolerance Gated through EZH2-Mediated Suppression of Trpc5 in Spinal GABAergic Interneurons in Male Mice. [Abstract]2025 Oct 20:e07908. PMID: 41111460 -
Biomaterials
Stiff extracellular matrix drives the differentiation of mesenchymal stem cells toward osteogenesis by the multiscale 3D genome reorganization. [Abstract]2024 Jul 27:312:122715. PMID: 39094522
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.
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Cell Rep Med
2025 Oct 27:102424. PMID: 41151579
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.
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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.
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Cell Mol Life Sci
Nuclear translocation of ISG15 regulated by PPP2R2B inhibits cisplatin resistance of bladder cancer. [Abstract]2024 Jul 8;81(1):292. PMID: 38976080 -
Biochem J
Chaetocin disrupts the SUV39H1-HP1 interaction independent of SUV39H1 methyltransferase activity. [Abstract]2023 Mar 31;480(6):421-432. PMID: 36896918 -
Breast Cancer
2022 Sep;29(5):854-868. PMID: 35553018 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Greiner D, et al. Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9. Nat Chem Biol. 2005 Aug;1(3):143-5. [Content Brief]
[2]. Tibodeau JD, et al. The anticancer agent chaetocin is a competitive substrate and inhibitor of thioredoxin reductase. Antioxid Redox Signal. 2009 May;11(5):1097-106. [Content Brief]
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 |
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