Chaetocin

Catalog No.S8068 Batch:S806804

Print

Technical Data

Formula

C30H28N6O6S4
Molecular Weight 696.84 CAS No. 28097-03-2
Solubility (25°C)* In vitro DMSO 25 mg/mL (35.87 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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]
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]

Protocol (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[4]
  • Cell lines

    HEK293T

  • Concentrations

    125 nM

  • Incubation Time

    24 h

  • Method

    Cells were treated with chaetocin (125 nM) or DMSO for 24 h.
Animal Study:

[2]
  • Animal Models

    Hur7 tumor-bearing mice, Hepa 1c1c-7 tumor-bearing mice

  • Dosages

    0.25 mg/kg

  • Administration

    i.p.

Selleck's Chaetocin has been cited by 25 publications

Inhibition of SUV39H1 reduces tumor angiogenesis via Notch1 in oral squamous cell carcinoma [ PeerJ, 2024, 12:e17222] PubMed: 38650654
G9a-targeted chaetocin induces pyroptosis of gastric cancer cells [ Asian Pac J Trop Bio, 2023;, 13(6): 268-276] PubMed: none
Methionine restriction promotes cGAS activation and chromatin untethering through demethylation to enhance antitumor immunity [ Cancer Cell, 2023, 41(6):1118-1133.e12] PubMed: 37267951
GalNAc-conjugated siRNA targeting the DNAJB1-PRKACA fusion junction in Fibrolamellar Hepatocellular Carcinoma [ Mol Ther, 2023, 10.1016/j.ymthe.2023.11.012] PubMed: 37980543
Oncogenic Addiction of Fibrolamellar Hepatocellular Carcinoma to the Fusion Kinase DNAJB1-PRKACA [ Clin Cancer Res, 2023, 29(1):271-278] PubMed: 36302174
Oncogenic Addiction of Fibrolamellar Hepatocellular Carcinoma to the Fusion Kinase DNAJB1-PRKACA [ Clin Cancer Res, 2023, 29(1):271-278] PubMed: 36302174
Priming therapy by targeting enhancer-initiated pathways in patient-derived pancreatic cancer cells [ EBioMedicine, 2023, 92:104602] PubMed: 37148583
Telomere dysfunction promotes cholangiocyte senescence and biliary fibrosis in primary sclerosing cholangitis [ JCI Insight, 2023, 10.1172/jci.insight.170320] PubMed: 37707950
Exposure to high-sugar diet induces transgenerational changes in sweet sensitivity and feeding behavior via H3K27me3 reprogramming [ Elife, 2023, 12e85365] PubMed: 37698486
Exposure to high-sugar diet induces transgenerational changes in sweet sensitivity and feeding behavior via H3K27me3 reprogramming [ Elife, 2023, 12e85365] PubMed: 37698486

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.