Azumamide E
Azumamide E is a HDAC inhibitor, with an IC50 of 0.064 μM against HDAC, 1.22 μM against HDAC1, and 2.28 μM against HDAC4. Azumamide E inhibits HDAC activity in nuclear extracts of leukemia cells and cervical adenocarcinoma cells. Azumamide E suppresses angiogenesis. Azumamide E is applicable for research on leukemia, cervical adenocarcinoma, and anti-angiogenesis.
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- CAS 番号: 585535-37-1
- 分子式: C27H38N4O6
- 分子量:514.62
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Help & FAQs
生物活性
製品説明
IC50 & Target
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HDAC1 1..22 μM (IC50) |
HDAC4 2.28 μM (IC50) |
体外実験
Azumamide E (Compound 5) potently inhibits HDAC activity in human leukemia K562 cells, with an IC50 of 0.064 μM[1].
Azumamide potently inhibits HDAC1 and HDAC4 enzymes prepared from 293T cells, with IC50 values of 1.22 μM and 2.28 μM, respectively, and does not inhibit HDAC6 at concentrations up to 50 μM[2].
Azumamide E (0-19 μM) exhibits dose-dependent anti-angiogenic activity in an in vitro vascular formation model using mouse induced pluripotent stem cells (iPS cells), with potent inhibitory effects observed at 1.9 μM and activity detectable at 0.19 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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CAS 番号 585535-37-1
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分子量 514.62
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分子式 C27H38N4O6
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配列
Cyclo({d-Ala}-{d-Phe}-{Oaa}-{d-Val})
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シーケンスの短縮
Cyclo(af-{Oaa}-v)
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Structure Classification
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Initial Source
Marine Sponge Mycale izuensis
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Human pluripotent stem cell endothelial-cell differentiation
Human pluripotent stem cell endothelial differentiation is based on stepwise developmental patterning: early activation of WNT/GSK3β inhibition promotes mesodermal or vascular progenitor entry, followed by endothelial specification using VEGF-related signaling, BMP4, FGF2, Notch modulation, or cAMP depending on the published protocol. Endothelial differentiation is read out by acquisition of CD31, CD34, VE-cadherin/CD144, KDR/VEGFR2, vWF, Tie2, NOS3, acetylated LDL uptake, tube/network formation, barrier function, and in vivo vessel-forming capacity where tested.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Vascular/Branching Fractal Analysis
Vascular/branching fractal analysis quantifies the geometric complexity of vessel trees or vascular networks from segmented 2D images, commonly by converting vessels into binary and/or skeletonized maps and estimating fractal dimension using box-counting or related approaches. Fractal dimension is interpreted as an image-derived readout of vascular branching complexity, space filling, or density, and has been applied to retinal photographs, fluorescein angiography, OCT angiography, capillary perfusion maps, and in vitro Matrigel angiogenesis networks. The assay readout is generated from vessel-positive pixels after image preprocessing, vessel segmentation, binarization, and optional skeletonization; reported outputs include fractal dimension, vessel density, branchpoint density, endpoint density, vessel length density, tortuosity, and generation-based branching metrics when VESGEN-style analysis is used. The biological interpretation is limited to quantitative vascular patterning and s
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Endothelial Tube Formation Assay
Endothelial tube formation assay evaluates the ability of endothelial cells to attach, migrate, align, and organize into capillary-like networks when cultured on gelled basement membrane extract or Matrigel; the readout is the morphology and quantity of tube-like networks, which reflects an in vitro endothelial morphogenesis step related to angiogenesis. Basement membrane extract/Matrigel provides laminin-rich extracellular matrix cues that support endothelial differentiation into capillary-like structures, but it can contain biologically active growth factors, so growth-factor-reduced matrix is preferred when testing defined angiogenic stimulators or inhibitors.
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Endothelial Cell Migration/Angiogenic Sprouting Assay
Endothelial cell migration and angiogenic sprouting assays are in vitro (and partially ex vivo-adapted) functional models that quantify the ability of endothelial cells to undergo coordinated migration, extracellular matrix invasion, and multicellular organization into capillary-like sprouts in response to pro-angiogenic stimuli such as VEGF, bFGF, or conditioned microenvironments. These assays are used to model early angiogenic events including tip-cell formation, directional migration, and lumen-like sprout extension, which collectively reflect angiogenic activation and vascular morphogenesis processes observed in vivo.
純度とドキュメンテーション
参考文献
[1]. Nakao Y, et al. Azumamides A-E: histone deacetylase inhibitory cyclic tetrapeptides from the marine sponge Mycale izuensis. Angew Chem Int Ed Engl. 2006 Nov 20;45(45):7553-7. [Content Brief]
[2]. Nakao Y, et al. Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells. Bioorg Med Chem Lett. 2008;18(9):2982-2984. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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