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BU-4061T

Epoxomicin

CAS: 134381-21-8

Molecular Formula: C28H50N4O7

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BU-4061T - Names and Identifiers

Name Epoxomicin
Synonyms BU-4061T
Aids010837
EPOXOMICIN
Epoxomicin
Aids-010837
EPOXOMICIN, SYNTHETIC
(2R)-2-[ACETYL-(N-METHYL-L-ISOLEUCYL)-L-ISOLEUCYL-L-THREONYL-L-LEUCYL]-2-METHYLOXIRANE
n-acetyl-n-methyl-l-isoleucyl-l-isoleucyl-n-[(1s)-3-methyl-1-[[(2r)-2-methyloxiranyl]carbonyl]butyl]-l-threoninamide
L-Threoninamide, N-acetyl-N-methyl-L-isoleucyl-L-isoleucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-
CAS 134381-21-8
InChIKey DOGIDQKFVLKMLQ-JTHVHQAWSA-N

BU-4061T - Physico-chemical Properties

Molecular FormulaC28H50N4O7
Molar Mass554.72
Melting Point107-109°
Specific Rotation(α)D24.5 -66.1 ± 0.4° (c = 0.5 in MeOH)
Solubility Soluble in DMSO (up to 10 mg/ml).
Appearancesolid
ColorWhite
Storage Condition-20°C
StabilityStable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
In vitro studyEpoxomicin 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 studyEpoxomicin 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.

BU-4061T - Risk and Safety

WGK Germany3
HS Code29299090

BU-4061T - Preparation solution concentration reference

 1mg5mg10mg
1 mM1.803 ml9.014 ml18.027 ml
5 mM0.361 ml1.803 ml3.605 ml
10 mM0.18 ml0.901 ml1.803 ml
5 mM0.036 ml0.18 ml0.361 ml
Last Update:2024-01-02 23:10:35

BU-4061T - 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
TargetValue
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
BU-4061T
Supplier List
Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: Epoxomicin Visit Supplier Webpage Request for quotation
CAS: 134381-21-8
Tel: +86-18821248368
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SKYRUN INDUSTRIAL CO.,LTD
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CAS: 134381-21-8
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Shanghai Yuanye Bio-Technology Co., Ltd.
Spot supply
Product Name: Epoxomicin Visit Supplier Webpage Request for quotation
CAS: 134381-21-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: Epoxomicin Visit Supplier Webpage Request for quotation
CAS: 134381-21-8
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Shanghai Amole Biotechnology Co., Ltd.
Spot supply
Product Name: Epoxomicin Request for quotation
CAS: 134381-21-8
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: Epoxomicin Visit Supplier Webpage Request for quotation
CAS: 134381-21-8
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Spot supply
Product Name: Epoxomicin Visit Supplier Webpage Request for quotation
CAS: 134381-21-8
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
SKYRUN INDUSTRIAL CO.,LTD
Spot supply
Product Name: EPOXOMICIN Visit Supplier Webpage Request for quotation
CAS: 134381-21-8
Tel: +86 0571-86722205
Email: sales@chinaskyrun.com
Mobile: +8618958170122
QQ: 2531159185 Click to send a QQ messageSend QQ message
Wechat: chinaskyrun
Shanghai Yuanye Bio-Technology Co., Ltd.
Spot supply
Product Name: Epoxomicin Visit Supplier Webpage Request for quotation
CAS: 134381-21-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
View History
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