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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 733035-26-2
- 分子式: C28H34N2O4
- 分子量:462.58
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Cathepsin アイソフォーム固有の製品をすべて表示
MoreParasite アイソフォーム固有の製品をすべて表示
MoreEndogenous Metabolite アイソフォーム固有の製品をすべて表示
More
生物活性
|
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.
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Cell Line:human hepatoma HepG2 cells
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Concentration:10-15 μM
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Incubation Time:24 h
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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 |
化学情報
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CAS 番号 733035-26-2
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性状 Solid
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分子量 462.58
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分子式 C28H34N2O4
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Color Off-white to gray
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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
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別名
ECO-4601; TLN-4601; BU 4664L
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
純度とドキュメンテーション
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データシート (273 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
- 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