28097-03-2
Chaetocin from Chaetomium minutum
CAS: 28097-03-2
Molecular Formula: C30H28N6O6S4
28097-03-2 - Names and Identifiers
| Name | Chaetocin from Chaetomium minutum |
| Synonyms | chetocin Chaetocin Chaetocin A CHAETOCIN(SH) HMTase Inhibitor II, Chaetocin CHAETOCIN FROM CHAETOMIUM MINUTUM Chaetocin from Chaetomium minutum |
| CAS | 28097-03-2 |
| EINECS | 200-258-5 |
| InChIKey | PZPPOCZWRGNKIR-PNVYSBBASA-N |
28097-03-2 - Physico-chemical Properties
| Molecular Formula | C30H28N6O6S4 |
| Molar Mass | 696.84 |
| Density | 1.87±0.1 g/cm3(Predicted) |
| Solubility | Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 25 mg/ml). |
| Appearance | White to off-white solid |
| Color | White |
| pKa | 12.39±0.10(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| MDL | MFCD00133163 |
| In vitro study | In Drosophila tissue culture cells SL-2, Chaetocin inhibited the activity of SU(VAR)3-9 and the number of dual methylation of the Lys9 site of H3, while inhibiting cell growth. In HepG2,Hep3B and Huh7 human hepatoma cells, Chaetocin inhibited the hypoxia response mediated by HIF-1. Chaetocin also effectively inhibited the proliferation of many tumor cells and the formation of clones with an IC50 of 2-10 nM. |
| In vivo study | Chaetocin (0.25 mg/kg, I. p.) inhibited tumor growth by down-regulating HIF-1[alpha]-mediated angiogenesis in a Hepa 1c1c-7 transplanted tumor mouse model. chaetocin(0.25 mg/kg, I. p.) significantly slowed tumor growth and produced little toxicity in a SKOV3 tumor-transplanted mouse model. |
28097-03-2 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. |
| UN IDs | 1544 |
| WGK Germany | 3 |
| RTECS | FM3032000 |
| HS Code | 29419090 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
28097-03-2 - Reference Information
| Overview | pilotesetin is one of the first natural metabolites isolated from the genus trichosanthis, it belongs to epithiodione pyrazine complex, which has received much attention because of its special biological activity. Studies have shown that trichlocetin is a specific inhibitor of histone methyltransferases Su(VAR)3-9 and G9a in eukaryotic cells, which can change the chromatin structure of cells and affect the epigenetic regulation of cells, thereby altering the expression of some important genes in the cell. Chaetin is a specific inhibitor of histone 9 lysine trimethylation (H3K9-Me3) transfer transferase SU(VAR)3-9, transcription and expression of genes can be regulated by regulating the methylation of histones. In some tumor cells, trichosanthin can affect the expression of several genes closely related to tumor growth, so it has potential clinical value in tumor therapy. |
| Application | Application of pilotesin in the preparation of drugs for the prevention and treatment of diabetes. The experimental results show that the hair shell can effectively correct glucose metabolism disorder, reduce blood sugar, improve islet B cell function, improve insulin resistance, enhance immune function, and the experimental results show that, chitin can effectively reduce serum total cholesterol, triglyceride, serum free fatty acid and urinary albumin, has good anti-lipid peroxidation, and can improve the activity of alanine aminotransferase, and the hair Shell also has a very good improvement of blood rheology, prevent or delay the role of atherosclerosis, can be used for the prevention and treatment of diabetic cardiovascular disease, such as the prevention and treatment of diabetes complicated with heart disease. And the experimental process, no obvious adverse reactions, is expected to develop into a new generation of safe and effective, prevention and treatment of diabetes. |
| biological activity | Chaetocin, a natural product from the genus Chaetocin, is a histone methyltransfer inhibitor, its IC50 for dSU(VAR)3-9, mouse G9a and Streptomyces crassa DIM5 were 0.8 μm, 2.5 μm and 3 μm, respectively. Chaetocin is an anti-cancer drug and an inhibitor of thioredoxin reduction (TrxR). |
| Target | TargetValue dSU(VAR)3-9 () 0.8 μm mouse G9a () 2.5 μm neuropora crassa DIM5 () 3 μm |
| Target | Value |
| dSU(VAR)3-9 () | 0.8 μM |
| mouse G9a () | 2.5 μM |
| Neurospora crassa DIM5 () | 3 μM |
| in vitro study | in Drosophila tissue culture cells SL-2, Chaetocin inhibited SU(VAR). 3-9 activity and the number of double methylation of the Lys9 site of H3, while inhibiting cell growth. In HepG2,Hep3B and Huh7 human hepatoma cells, Chaetocin inhibited the hypoxia response mediated by HIF-1. Chaetocin also effectively inhibited the proliferation of many tumor cells and the formation of clones with an IC50 of 2-10 nM. |
| in vivo study | in a mouse model of Hepa 1c1c-7 transplanted tumor, Chaetocin (0.25 mg/kg, I. p.) tumor growth was inhibited by down-regulating HIF-1[alpha]-mediated angiogenesis. chaetocin(0.25 mg/kg, I. p.) significantly slowed tumor growth and produced little toxicity in a SKOV3 tumor-transplanted mouse model. |
Last Update：2024-04-09 21:22:08
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