1. Epigenetics
  2. Histone Methyltransferase

Chaetocin 

Cat. No.: HY-N2019 Purity: >98.0%
Handling Instructions

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.
Chaetocin Chemical Structure

Chaetocin Chemical Structure

CAS No. : 28097-03-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 828 In-stock
1 mg USD 180 In-stock
5 mg USD 540 In-stock
10 mg USD 972 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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]

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].

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].

References
Preparing Stock Solutions
Concentration Volume 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.
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
Molecular Weight

696.84

Formula

C₃₀H₂₈N₆O₆S₄

CAS No.

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 26 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: >98.0%

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Product Name:
Chaetocin
Cat. No.:
HY-N2019
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