Diazepinomicin
Diazepinomicin (ECO-4601) is an anticancer and antibacterial agent. Diazepinomicin can be produced by a Micromonospora strain. Diazepinomicin induces Apoptosis. Diazepinomicin inhibits the proteases Rhodesain and Cathepsin L at an IC50 of 70-90 μM. Diazepinomicin possesses anti-inflammatory and anti-tumor activity. Diazepinomicin has demonstrated activity against hepatocellular carcinoma. Diazepinomicin shows antiparasitic activity against trypomastigote forms of Trypanosoma brucei with an IC50 of 13.5 μM. Diazepinomicin exhibits moderate antibacterial activity against specific Gram-positive bacteria, with an MIC of approximately 32 μg/mL.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 733035-26-2
- Formel: C28H34N2O4
- Molecular Weight:462.58
-
Speicherung:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Alle Cathepsin Isoform-spezifische Produkte anzeigen
MoreAlle Parasite Isoform-spezifische Produkte anzeigen
MoreAlle Endogenous Metabolite Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
|
Microbial Metabolite |
Trypanosoma |
cathepsin L 70-90 μM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
0.43 μg/mL
Compound: 1, BU-4664L
|
Antiinvasive activity against HUVEC assessed as inhibition of cell migration after 6 hrs by Matrigel assay
Antiinvasive activity against HUVEC assessed as inhibition of cell migration after 6 hrs by Matrigel assay
|
[PMID: 20056543] |
| HUVEC | IC50 |
0.72 μg/mL
Compound: 1, BU-4664L
|
Antiangiogenic activity against HUVEC cells assessed as inhibition of vascular formation after 6 hrs by wound healing assay
Antiangiogenic activity against HUVEC cells assessed as inhibition of vascular formation after 6 hrs by wound healing assay
|
[PMID: 20056543] |
| HUVEC | IC50 |
2 μg/mL
Compound: 1, BU-4664L
|
Cytotoxicity against HUVEC cells
Cytotoxicity against HUVEC cells
|
[PMID: 20056543] |
| NCI-H460 | GI50 |
13.6 μM
Compound: 1; BU-4664L
|
Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition by MTT assay
|
[PMID: 34838651] |
| PC-3 | GI50 |
1.95 μM
Compound: 1; BU-4664L
|
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition by MTT assay
|
[PMID: 34838651] |
| Renca | IC50 |
0.78 μg/mL
Compound: 1, BU-4664L
|
Antiinvasive activity against mouse Renca by Matrigel assay
Antiinvasive activity against mouse Renca by Matrigel assay
|
[PMID: 20056543] |
| Renca | IC50 |
8.3 μg/mL
Compound: 1, BU-4664L
|
Cytotoxicity against mouse Renca cells
Cytotoxicity against mouse Renca cells
|
[PMID: 20056543] |
Diazepinomicin (1-25 μM; 24-72 h) induces dose-dependent antiproliferative activity in hepatocellular carcinoma HepG2 cells[1].
Diazepinomicin exhibits moderate antibacterial activity against specific Gram-positive bacteria, with an MIC of approximately 32 μg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:human hepatoma HepG2 cells
-
Concentration:10-15 μM
-
Incubation Time:24 h
-
Result:Induced clumping of cells with slight distortion, as well as very condensed and fragmented nuclei (hallmark features of apoptosis). Induced condensed nuclei and apoptotic bodies, characteristic of apoptotic cells. Induced DNA fragmentation, visualized as characteristic DNA ladder bands on agarose gel electrophoresis.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS. Nr. 733035-26-2
-
Appearance Solid
-
Molecular Weight 462.58
-
Formel C28H34N2O4
-
Color Off-white to gray
-
SMILES
O=C1C2=CC=CC(O)=C2NC3=C(O)C=C(O)C=C3N1C/C=C(C)/CC/C=C(C)/CC/C=C(C)\C
-
Synonyms
ECO-4601; TLN-4601; BU 4664L
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Reinheit & Dokumentation
-
Data Sheet (273 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Diazepinomicin Related Classifications
HY-N6674 Related Classifications
Powered by Bioz
- Diazepinomicin
- 733035-26-2
- ECO-4601
- TLN-4601
- BU 4664L
- ECO4601
- ECO 4601
- TLN4601
- TLN 4601
- TLN-4601
- Apoptosis
- Bacterial
- Cathepsin
- Parasite
- Endogenous Metabolite
- human hepatoma HepG2 cells
- Bcl2 protein
- BAX protein
- Gram-positive bacteria
- apoptotic nuclear condensation
- apoptotic body formation
- apoptosis
- DNA fragmentation
- human hepatoma cells
- hepatocellular carcinoma
- Inhibitor
- inhibitor
- inhibit