Chaetocin

SKU: orb1685550

Description

Chaetocin is a fungal metabolite and potent histone methyltransferase inhibitor, exhibiting IC50 values of 0.8 μM, 2.5 μM, and 3 μM against dSU(VAR)3-9, mouse G9a, and DIM5, respectively. It is widely used in epigenetics research to probe histone methylation's role in gene silencing, cancer, and differentiation in both cellular and animal models.

Research Area

Epigenetics & Chromatin, Infectious Disease & Virology

Key Properties

• CAS Number: 28097-03-2
• MW: 696.84
• Purity: 98.82% (May vary between batches)
• Formula: C₃₀H₂₈N₆O₆S₄
• SMILES: CN1C(=O)C23CC4(C(Nc5ccccc45)N2C(=O)C1(CO)SS3)C12CC34SSC(CO)(N(C)C3=O)C(=O)N4C1Nc1ccccc21
• Target: Histone Methyltransferase,Antibiotic,Antibacterial
• Solubility: DMSO:7 mg/mL (10.05 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  dSU(VAR)3-9:0.8 μM|G9a (mouse):2.5 μM|DIM5 (neurospora crassa):3 μM
• In Vivo:
  In Hepa 1c1c-7 tumor-bearing mice, Chaetocin (0.25 mg/kg, i.p.) inhibits tumor growth by deregulating HIF-1[alpha]-mediated angiogenesis. In SKOV3 tumor-bearing nude mice, chaetocin treatment (0.25 mg/kg, i.p.) significantly delays the tumor growth with minimal evidence of toxicities.
• In Vitro:
  In SL-2 Drosophila tissue culture cells, Chaetocin causes the inhibition of SU(VAR)3-9 and the number of H3 molecules dimethylated at Lys9, and also inhibits cell growth. In HepG2, Hep3B, and Huh7 human hepatoma cells, Chaetocin inhibits HIF-1-Mediated hypoxic responses. Chaetocin also potently inhibits proliferation and colony formation in a broad range of cancer cell lines with IC50 of 2-10 nM.
• Cell Research:
  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.

Storage & Handling

• Storage: store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Neurospora crassa DIM5, Inhibitor, inhibit, HistoneMethyltransferase, Histone Methyltransferase, mouse G9a, Bacterial, Antibiotic, Chaetocin, dSU(VAR)3-9

Compound Identifiers

PubChem CID

161591