EPOXOMICIN
Epoxomicin
CAS: 134381-21-8
Molecular Formula: C28H50N4O7
EPOXOMICIN - Names and Identifiers
EPOXOMICIN - Physico-chemical Properties
| Molecular Formula | C28H50N4O7 |
| Molar Mass | 554.72 |
| Melting Point | 107-109° |
| Specific Rotation(α) | D24.5 -66.1 ± 0.4° (c = 0.5 in MeOH) |
| Solubility | Soluble in DMSO (up to 10 mg/ml). |
| Appearance | solid |
| Color | White |
| Storage Condition | -20°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months. |
| In vitro study | Epoxomicin is covalently bound to LMP7, X, Mec1, and the Z catalytic subunit of the proteasome. Treatment of HUVECs with Epoxomicin (100 nM) increased p53 protein levels 30-fold. Epoxomicin (10 μm) acts on HeLa cells, resulting in accumulation of ubiquitinated proteins. Epoxomicin(10 μm) inhibited the degradation of IκBα in HeLa cells. Epoxomicin(10 μm) significantly reduced TNF-α stimulated NF-κB DNA binding activity in HeLa cells in a dose-dependent manner. Epoxomicin inhibited the proliferation of EL4 lymphoma cells with an IC50 of 4 nM. Epoxomicin(1 μm) reduced LCMV GP33 and enhanced gp276. Epoxomicin inhibits Babesia bigemina growth with an IC50 of 4 nM. At the doses of 0.5 mg/kg and 0.05 mg/kg of Epoxomicin treated B. microti, the peak values of haematoxemia were 34.8% and 42.3%, respectively. Treatment of plasma falciparum with Epoxomicin (100 nM) reduced by 78%, 86%, and 77% in hematoxia. Epoxomicin (10 μm) inhibits the formation of oocysts from gametes and gametes in Anopheles mosquitoes. |
| In vivo study | Epoxomicin daily at a dose of 0.58 mg/kg reduced the CS response by 44% compared to blank control mice. Mice were treated with Epoxomicin (2.9 mg/kg) and ear swelling was measured 24 hours later, effectively inhibiting 95% of the irritation-related inflammatory response. |
EPOXOMICIN - Risk and Safety
| WGK Germany | 3 |
| HS Code | 29299090 |
EPOXOMICIN - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.803 ml | 9.014 ml | 18.027 ml |
| 5 mM | 0.361 ml | 1.803 ml | 3.605 ml |
| 10 mM | 0.18 ml | 0.901 ml | 1.803 ml |
| 5 mM | 0.036 ml | 0.18 ml | 0.361 ml |
Last Update：2024-01-02 23:10:35
EPOXOMICIN - Reference Information
| biological activity | Epoxomicin (BU-4061T, Aids010837) is a selective proteasome inhibitor with anti-inflammatory activity, primarily inhibiting the CH-L activity of 20S proteasome, as well as the catalytic activity of T-L and PGPH. Epoxomicin can promote apoptosis. |
| target | TargetValue 20S proteasome |
| Target | Value | In vitro study | Epoxomicin covalently bound to the Z catalytic subunit of LMP7, X, MECL1, and proteasome. Epoxomicin (100 nM) treatment of HUVECs increased p53 protein level by 30 times. Epoxomicin (10 μM) acts on HeLa cells, resulting in accumulation of ubiquitinated proteins. Epoxomicin(10 μM) acted on HeLa cells and inhibited IκBα degradation. Epoxomicin(10 μM) acts on HeLa cells, significantly reducing TNF-α-stimulated NF-κB DNA binding activity, which is dose-dependent. Epoxomicin inhibited the proliferation of EL4 lymphoma cells with IC50 of 4 nM. Epoxomicin(1 μM) reduced LCMV GP33 and enhanced GP276. Epoxomicin inhibited the growth of Babesia bigemina with IC50 of 4 nM. Epoxomicin B. microti was treated with 0.5 mg/kg and 0.05 mg/kg doses, and the peak value of bacteremia was 34.8% and 42.3% respectively. Epoxomicin (100 nM) treatment Plasmodium falciparum, reducing 78%, 86% and 77% of bacteremia. Epoxomicin (10 μM) inhibited gametes and small gametes to form the oocysts of Anopheles mosquitoes. |
| in vivo study | Epoxomicin were treated at a daily dose of 0.58 mg/kg, which reduced 44% CS response compared with blank control mice. Mice were treated with Epoxomicin (2.9 mg/kg). After 24 hours, ear swelling was measured to effectively inhibit 95% irritation-related inflammatory response. |
Last Update：2024-04-10 22:29:15
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Product Name: Epoxomicin Visit Supplier Webpage Request for quotationCAS: 134381-21-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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