Chaetocin
Chaetocin structure
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Common Name | Chaetocin | ||
|---|---|---|---|---|
| CAS Number | 28097-03-2 | Molecular Weight | 696.840 | |
| Density | 1.9±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C30H28N6O6S4 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
| Symbol |
GHS07 |
Signal Word | Warning | |
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Inhibition of histone H3K9 methyltransferases by gliotoxin and related epipolythiodioxopiperazines.
J. Antibiot. 65(5) , 263-5, (2012)
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Individual epigenetic status of the pathogenic D4Z4 macrosatellite correlates with disease in facioscapulohumeral muscular dystrophy.
Clin. Epigenetics. 7(1) , 37, (2015) Both forms of facioscapulohumeral muscular dystrophy (FSHD) are associated with aberrant epigenetic regulation of the chromosome 4q35 D4Z4 macrosatellite. Chromatin changes due to large deletions of heterochromatin (FSHD1) or mutations in chromatin regulatory... |
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Epidithiodiketopiperazine as a pharmacophore for protein lysine methyltransferase G9a inhibitors: reducing cytotoxicity by structural simplification.
Bioorg. Med. Chem. Lett. 23(3) , 733-6, (2013) Chaetocin (1), a structurally complex epidithiodiketopiperazine (ETP) alkaloid produced by Chaetomium minutum, is a potent inhibitor of protein lysine methyltransferase G9a, which plays important roles in many biological processes. Here we present our synthet... |
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Unnatural enantiomer of chaetocin shows strong apoptosis-inducing activity through caspase-8/caspase-3 activation.
Bioorg. Med. Chem. Lett. 20(17) , 5085-8, (2010) Chaetocin, a natural product isolated from Chaetomium species fungi, was reported to have various biological activities, including antitumor and antifungal activities. Recently, we reported the first total synthesis of chaetocin and its derivatives. Here, we ... |
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Epigenetic regulation of HIV-1 transcription.
Epigenomics 3(4) , 487-502, (2011) After entry into the target cell and reverse transcription, HIV-1 genes are integrated into the host genome. It is now well established that the viral promoter activity is directly governed by its chromatin environment. Nuc-1, a nucleosome located immediately... |
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Remodeling of nuclear architecture by the thiodioxoxpiperazine metabolite chaetocin.
Exp. Cell Res. 316(10) , 1662-80, (2010) Extensive changes of higher order chromatin arrangements can be observed during prometaphase, terminal cell differentiation and cellular senescence. Experimental systems where major reorganization of nuclear architecture can be induced under defined condition... |
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Role of the histone H3 lysine 9 methyltransferase Suv39 h1 in maintaining Epsteinn-Barr virus latency in B95-8 cells.
FEBS J. 281(9) , 2148-58, (2014) The ability of Epstein-Barr Virus (EBV) to establish latent infection is associated with infectious mononucleosis and a number of malignancies. In EBV, the product of the BZLF1 gene (ZEBRA) acts as a master regulator of the transition from latency to the lyti... |
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Improved therapeutic effect against leukemia by a combination of the histone methyltransferase inhibitor chaetocin and the histone deacetylase inhibitor trichostatin A.
J. Korean Med. Sci. 28(2) , 237-46, (2013) SUV39H1 is a histone 3 lysine 9 (H3K9)-specific methyltransferase that is important for heterochromatin formation and the regulation of gene expression. Chaetocin specifically inhibits SUV39H1, resulted in H3K9 methylation reduction as well as reactivation of... |
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Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.
Nat. Chem. Biol. 1 , 143, (2005) Histone methylation plays a key role in establishing and maintaining stable gene expression patterns during cellular differentiation and embryonic development. Here, we report the characterization of the fungal metabolite chaetocin as the first inhibitor of a... |
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The anticancer agent chaetocin is a competitive substrate and inhibitor of thioredoxin reductase.
Antioxid. Redox Signal. 11 , 1097-1106, (2009) We recently reported that the antineoplastic thiodioxopiperazine natural product chaetocin potently induces cellular oxidative stress, thus selectively killing cancer cells. In pursuit of underlying molecular mechanisms, we now report that chaetocin is a comp... |