Cat. No.: HY-N2019

Chaetocin

Name: Chaetocin
Brand: MedChemExpress
SKU: HY-N2019
Price: 160.00 USD
Availability: InStock
Rating: 5 (11 reviews)

11 Cited Publications

고객리뷰

Based on 11 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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.22%
CAS No.: 28097-03-2
화학식: C₃₀H₂₈N₆O₆S₄
분자량:696.84

보관:

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

Chaetocin Chemical Structure

CAS No.: 28097-03-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (11)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

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

All Histone Methyltransferase Isoforms :

All Antibiotic Isoforms :

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]
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]
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]
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.

Chemical Information

CAS No. 28097-03-2
Appearance Solid
분자량 696.84
화학식 C₃₀H₂₈N₆O₆S₄
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
- Alkaloids
- Alkaloid Dimers
Initial Source
- Microorganisms
Chaetomium species
선적

Room temperature in continental US; may vary elsewhere.

보관

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

Publications (11)

All Cell Imaging/StainingRT-PCRCell Proliferation/Viability AssayFlow CytometryIn Vivo Efficacy Study

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Journal Impact Factor

Autophagy

Autophagy regulates the maternal-to-zygotic transition through MAP1LC3B-mediated maternal mRNA decay. [Abstract]

2026 Feb;22(2):285-297. PMID: 41231099
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.
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
Cell Rep Med

Ribosome dysregulation and intervention in age-related infertility. [Abstract]

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.
Biomaterials

Stiff extracellular matrix drives the differentiation of mesenchymal stem cells toward osteogenesis by the multiscale 3D genome reorganization. [Abstract]

2025 Jan:312:122715. PMID: 39094522

Chaetocin purchased from MedChemExpress. Usage Cited in: Biomaterials. 2025 Jan:312:122715. [Abstract]

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

06 May 2022.

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.
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

Overexpression of MCAM induced by SMYD2-H3K36me2 in breast cancer stem cell properties. [Abstract]

2022 Sep;29(5):854-868. PMID: 35553018
bioRxiv

2026 Sep 17:2026.09.11.751063. PMID: 42779618
Research Square Print

September 20th, 2022.

용액&용해도

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
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)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

Chaetocin

11 Cited Publications

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Chaetocin

Publications Citing Use of MedChemExpress (MCE) Chaetocin

All Histone Methyltransferase Isoforms

All Antibiotic Isoforms