Diazepinomicin
Diazepinomicin (ECO-4601) is a reagent with both anticancer and antibacterial activities.. Diazepinomicin decreases Bcl2 and BAX expression, induces dose-dependent cell death and apoptotic bodies, and inhibits Ras-MAPK signaling and tumor growth/proliferation. Diazepinomicin induces apoptosis through caspase 3 activation, PARP cleavage, cytochrome C release, loss of membrane potential, and DNA fragmentation, independent of PBR expression. Diazepinomicin binds PBR/TSPO and displaces PK11195 through its farnesyl side chain rather than the dibenzodiazepinone core. Diazepinomicin can be used in research on hepatocellular carcinoma, Gram-positive bacterial infections, and glioma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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生物活性
製品説明
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BCL2 |
PBR |
Bax |
Ras |
p38 MAPK |
Caspase 3 |
PARP |
TSPO |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
0.43 μg/mL
Compound: 1, BU-4664L
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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
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[PMID: 20056543] |
| HUVEC | IC50 |
0.72 μg/mL
Compound: 1, BU-4664L
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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
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[PMID: 20056543] |
| HUVEC | IC50 |
2 μg/mL
Compound: 1, BU-4664L
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Cytotoxicity against HUVEC cells
Cytotoxicity against HUVEC cells
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[PMID: 20056543] |
| NCI-H460 | GI50 |
13.6 μM
Compound: 1; BU-4664L
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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
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[PMID: 34838651] |
| PC-3 | GI50 |
1.95 μM
Compound: 1; BU-4664L
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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
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[PMID: 34838651] |
| Renca | IC50 |
0.78 μg/mL
Compound: 1, BU-4664L
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Antiinvasive activity against mouse Renca by Matrigel assay
Antiinvasive activity against mouse Renca by Matrigel assay
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[PMID: 20056543] |
| Renca | IC50 |
8.3 μg/mL
Compound: 1, BU-4664L
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Cytotoxicity against mouse Renca cells
Cytotoxicity against mouse Renca cells
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[PMID: 20056543] |
体外実験
Diazepinomicin (10-15 μM; 24 h) induces apoptotic nuclear condensation and apoptotic body formation in human hepatoma HepG2 cells[1].
Diazepinomicin (10-15 μM; 24 h) induces DNA fragmentation (a hallmark of apoptosis) in human hepatoma HepG2 cells[1].
Diazepinomicin (10-15 μM; 24 h) downregulates the expression of 25 kDa Bcl-2 and 20 kDa BAX proteins in human hepatoma HepG2 cells[1].
Diazepinomicin (10 µM; 0-6 h) induces cytochrome C release from mitochondria to cytosol between 2 and 4 h in both Jurkat WT and Jurkat-PBR cells[3].
Diazepinomicin (10 µM; 0-24 h) induces DNA nucleosomal fragmentation and more than 95% cell death by 24 h in both Jurkat WT and Jurkat-PBR cells[3].
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:1; 2; 5; 10; 25 μM
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Incubation Time:24 h
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Result:Induced dose-dependent decreases in HepG2 cell proliferation, with increasing cell death observed at higher concentrations.
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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).\nInduced condensed nuclei and apoptotic bodies, characteristic of apoptotic cells.\nInduced DNA fragmentation, visualized as characteristic DNA ladder bands on agarose gel electrophoresis.
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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:Reduced intensity of Bcl-2 (25 kDa) and BAX (20 kDa) protein bands, indicating downregulation of both anti-apoptotic Bcl-2 and pro-apoptotic BAX protein expression.
- Research Protocol for Infectious Diseases
- RNA extraction experimental
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- Liver Cancer Modeling
- Gram Staining of Tissue Sections
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Fluorescent plasma-membrane potential dye assay
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
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 (278 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
[2]. Charan RD, et al. Diazepinomicin, a new antimicrobial alkaloid from a marine Micromonospora sp. J Nat Prod. 2004;67(8):1431-1433. [Content Brief]
[3]. Bertomeu T, et al. TLN-4601 peripheral benzodiazepine receptor (PBR/TSPO) binding properties do not mediate apoptosis but confer tumor-specific accumulation. Biochemical pharmacology. 2010 Nov 15;80(10):1572-9. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Diazepinomicin 関連分類
HY-N6674 関連分類
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Keywords
- Diazepinomicin
- 733035-26-2
- ECO-4601
- TLN-4601
- BU 4664L
- ECO4601
- ECO 4601
- TLN4601
- TLN 4601
- TLN-4601
- Apoptosis
- Bacterial
- Caspase
- PARP
- TSPO
- Bcl-2 Family
- Ras
- p38 MAPK
- poly ADP ribose polymerase
- Translocator Protein
- BAX
- Bcl2
- Gram-positive bacterial infection
- PBR/TSPO
- Ras-MAPK signaling
- apoptosis
- blood-brain barrier
- caspase 3
- glioma
- hepatocellular carcinoma
- Inhibitor
- inhibitor
- inhibit