2. Apoptosis Anti-infection Metabolic Enzyme/Protease
  3. Apoptosis Bacterial Cathepsin Parasite Endogenous Metabolite
  4. Diazepinomicin

Diazepinomicin  (Synonyms: ECO-4601; TLN-4601; BU 4664L)

Cat. No.: HY-N6674
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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.

For research use only. We do not sell to patients.

Diazepinomicin

Diazepinomicin Chemical Structure

CAS No. : 733035-26-2

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Diazepinomicin Related Antibodies

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Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

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Human Endogenous Metabolite Microbial Metabolite

  • Biological Activity

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Description

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[1][2].

IC50 & Target[1]

Microbial Metabolite

 

Trypanosoma

 

cathepsin L

70-90 μM (IC50)

Cellular Effect
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]
In Vitro

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.

Diazepinomicin Related Antibodies

Apoptosis Analysis[1]

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.
Clinical Trial
Molecular Weight

462.58

Formula

C28H34N2O4
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Purity & Documentation
References
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Diazepinomicin Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Diazepinomicin733035-26-2ECO-4601 TLN-4601 BU 4664LECO4601ECO 4601TLN4601TLN 4601TLN-4601ApoptosisBacterialCathepsinParasiteEndogenous Metabolitehuman hepatoma HepG2 cellsBcl2 proteinBAX proteinGram-positive bacteriaapoptotic nuclear condensationapoptotic body formationapoptosisDNA fragmentationhuman hepatoma cellshepatocellular carcinomaInhibitorinhibitorinhibit

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