Home Epigenetics Histone Methyltransferase inhibitor - G9a/GLP inhibitor - Anti-infection inhibitor - Thioredoxin Reductase inhibitor Chaetocin For research use only.

Chaetocin

Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR).

Chaetocin Chemical Structure

Chaetocin Chemical Structure

CAS No. 28097-03-2

Purity & Quality Control

Chaetocin Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 Cytotoxicity assay Cytotoxicity against human A549 cells, IC50 = 0.025 μM. 20303767
Hep3b Function assay Inhibition of HIF-1alpha-mediated VEGF expression in human Hep3b cells by luciferase reporter gene assay, IC50 = 0.04 μM. 22305612
Hep3b Function assay Inhibition of HIF-1alpha-mediated VEGF secretion in human Hep3b cells by ELISA, IC50 = 0.1 μM. 22305612
Jurkat Cytotoxicity assay 40 hrs Cytotoxicity against human Jurkat cells after 40 hrs bioluminescence assay, IC50 = 0.6 μM. 20303767
Drosophila melanogaster SL2 Function assay 0.1 uM 5 days Inhibition of SU(VAR)3-9 in Drosophila melanogaster SL2 cells assessed as reduction of H3K9me2 at 0.1 uM after 5 days by MALDI-TOF MS seeded at 2.5 million cells/ml density 16408017
Drosophila melanogaster SL2 Function assay 0.5 uM 5 days Inhibition of SU(VAR)3-9 in Drosophila melanogaster SL2 cells assessed as reduction of H3K9me2 at 0.5 uM after 5 days by MALDI-TOF MS seeded at 2.5 million cells/ml density 16408017
Drosophila melanogaster SL2 Function assay 0.5 uM Inhibition of SU(VAR)3-9 in Drosophila melanogaster SL2 cells assessed as reduction of H3K9me3 at 0.5 uM by immunostaining method 16408017
HL60 Apoptosis assay 30 uM 4 hrs Induction of apoptosis in human HL60 cells assessed as necrotic cell death at 30 uM after 4 hrs using DAPI/PI by confocal laser microscopy analysis 20675131
HL60 Apoptosis assay 0.3 uM 4 hrs Induction of apoptosis in human HL60 cells assessed as nuclear fragmentation at 0.3 uM after 4 hrs using DAPI/PI by confocal laser microscopy analysis 20675131
HL60 Apoptosis assay 0.3 uM 2 hrs Induction of apoptosis in human HL60 cells assessed as activation of caspase 3 at 0.3 uM after 2 hrs by Western blot analysis 20675131
MCF7 Function assay Inhibition of histone-lysine N-methyltransferase in human MCF7 cells assessed as decrease in methylation of RARbeta DNA by qPCR method ChEMBL
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Biological Activity

Description Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR).
Targets
dSU(VAR)3-9 [1] mouse G9a [1] Neurospora crassa DIM5 [1]
0.8 μM 2.5 μM 3 μM
In vitro
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. [1]

In HepG2, Hep3B, and Huh7 human hepatoma cells, Chaetocin inhibits HIF-1-Mediated hypoxic responses. [2]

Chaetocin also potently inhibits proliferation and colony formation in a broad range of cancer cell lines with IC50 of 2-10 nM. [3]
Kinase Assay Methylation assays
Unless otherwise stated, reactions are performed as followed: 1 g of purified enzyme (dSU(VAR)3-9 213; GST-hSUV39H1(82-412); GST-ncDIM5(19-318) and GSTmG9a(621-1000); dPRSET7(1-691); His-SET7/9(109-366) or enzyme complex expressed in a baculoviral expression system (dE(z), dSU(Z)12, dp55, dESC) were incubated for 30 minutes with 1 g of a peptide containing the first 19 amino acids of H3 plus an additional cystein residue (ARTKQTARKSTGGKAPRKQC) in a total volume of 40μl in BC25 (10mM HEPES pH7.6, 25mM NaCl, 1mM EDTA, 10%glycerol). All enzymes except for the E(z) complex had a similar specific activity between 5-10 nmole/min/mg. For the E(z) complex, the specific activity is approximately 5-10 fold lower, which is probably due to an incomplete formation of the full complex that is required for the highest activity. As a methyl donor S-Adenosyl [methyl-3H] methionine (SAM) is present in the reaction at a final concentration of 40 M with a specific activity of 0.3Ci/mmole. Reactions are stopped by adding 1/10 volume of 100% acetic acid and the incorporation of radioactivity is measured by spotting 30 l of the reaction on P81 filter paper and subsequent scintillation counting. For the inhibitor screening, 1 l of inhibitor with a concentration of 10 g/l is added to each reaction. In the cases where PRSET7 or the E(z) complex is used as enzyme either recombinant nucleosomes (1 g) or recombinant H3 (1 g) respectively replaced the H3 peptide as a substrate.
Cell Research Cell lines HEK293T
Concentrations 125 nM
Incubation Time 24 h
Method

Cells were treated with chaetocin (125 nM) or DMSO for 24 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Procaspase-3 / Cleaved Caspase-3 / PARP 26890137
Growth inhibition assay Cell viability 18176557
In Vivo
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. [2]

In SKOV3 tumor-bearing nude mice, chaetocin treatment (0.25 mg/kg, i.p.) significantly delays the tumor growth with minimal evidence of toxicities. [3]
Animal Research Animal Models Hur7 tumor-bearing mice, Hepa 1c1c-7 tumor-bearing mice
Dosages 0.25 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 696.84 Formula

C30H28N6O6S4
CAS No. 28097-03-2 SDF Download Chaetocin SDF
Smiles CN1C(=O)C23CC4(C(N2C(=O)C1(SS3)CO)NC5=CC=CC=C54)C67CC89C(=O)N(C(C(=O)N8C6NC1=CC=CC=C71)(SS9)CO)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 25 mg/mL ( (35.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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