Chaetocin

Name: Chaetocin
Brand: MedChemExpress
SKU: HY-N2019
Rating: 5.0 (10 reviews)

Cat. No.: HY-N2019 Purity: 99.22%: Data Sheet
COA

SDS
Handling Instructions
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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.

CAS No. : 28097-03-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 10 publication(s) in Google Scholar

10 Publications Citing Use of MCE Chaetocin

Cell Imaging/Staining

RT-PCR

Cell Proliferation/Viability Assay

Flow Cytometry

In Vivo Efficacy Study

: 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 0.6 μM (HMT)^[1], 4 μM (TrxR)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	< 0.025 μM Compound: 12	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 20303767]
HL-60	IC₅₀	0.127 nM 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 nM 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 μM 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 μM 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 nM 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 nM 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 nM 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 nM 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]

In Vitro

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.

In Vivo

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.

Molecular Weight

696.84

Formula

C₃₀H₂₈N₆O₆S₄

CAS No.

28097-03-2

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

Microorganisms

Chaetomium species

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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.

Purity & Documentation

Purity: 99.58%

Select Batch:

Data Sheet (280 KB) SDS (392 KB)

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

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]

Cell Assay
^[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 has not independently confirmed the accuracy of these methods. They are for reference only.

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

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

Chaetocin Related Classifications

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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Chaetocin

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Chaetocin Related Antibodies

10 Publications Citing Use of MCE Chaetocin

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Chaetocin Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

Chaetocin Related Classifications

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