Squalamine
Based on 1 publication(s) in Google Scholar
Squalamine (MSI-1256) is an aminosterol compound with broad-spectrum antiviral activity. Squalamine makes cells less conducive to certain viral replication by altering the electrostatic interactions in the inner membrane of host cells. Squalamine also has antibacterial and antitumor activities. Squalamine has broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria, fungi and protozoa. Squalamine inhibits tumor-related angiogenesis and the growth of human breast cancer cells. Squalamine restores the function of enteric nervous system in Parkinson,s disease mouse models.
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- Reinheit : 98.38%
- CAS. Nr.: 148717-90-2
- Formel: C34H65N3O5S
- Molecular Weight:627.96
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) Squalamine
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Biologische Aktivität
Beschreibung
In Vitro
Squalamine (0-100 μg/mL; 2 h) inhibits dengue virus (Den V2) infection in HMEC-1 cells, and dengue infection is suppressed by about 60% at 40 μg/mL and completely suppressed at 100 μg/mL[1].
Squalamine (0-20 μg/mL; 16 h) effectively inhibits the replication of human hepatitis B virus (HBV) in human primary hepatocytes[1].
Squalamine (0.16-3.2 μM; 8 days) inhibits VEGF-induced proliferation of vascular endothelial cells HUVEC in a dose-dependent manner, but has no direct inhibitory effect on the proliferation of human breast MCF-7 cancer cells[2].
Squalamine (0.001-1 μM; 1 h) blocks FAK phosphorylation in HUVECs exposed to VEGF[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HUVEC cells
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Concentration:0.001, 0.01, 0.1 and 1 μM
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Incubation Time:1 h
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Result:Inhibited the phosphorylation levels of FAK in a concentration‐dependent manner
In Vivo
Squalamine (20 mg; Single application; 0-3 days) has a decolonizing effect on S. aureus on the skin in a mouse model[3].
Squalamine (20-120 mg/kg; Oral gavage; 5 days) restores the function of the mesenteric nervous system in PD mouse models[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic mice aged 6 weeks old bearing breast tumor xenografts[2]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection (i.p.); 28 days
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Result:Significantly retarded the growth of tumors, but the combination with Trastuzumab (HY-P9907) was more effective.
Suppressed MCF-7/HER-2 breast xenograft-associated angiogenesis.
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Animal Model:10 μL S. aureus suspension(108 cfu/mL) was applied to the female BALB/c mice skin[3]
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Dosage:20 mg
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Administration:Single application; 3 days
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Result:Reduced S. aureus viable cells by up to 4 log after two days compared with the control.
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Animal Model:PD mice models ( hSNCAA53T mice and PrP-A53T human α-syn overexpressing transgenic mice)[4]
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Dosage:20, 40, 80, or 120 mg/kg
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Administration:Oral gavage (i.g.); 5 days
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Result:Effectively restored disordered colonic motility in PD mice models.
Increased colonic transit in PrP-A53T mice.
Reduced myenteric intrinsic primary afferent neuron excitability in hSNCAA53T mice.
Chemical Information
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CAS. Nr. 148717-90-2
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Appearance Solid
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Molecular Weight 627.96
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Formel C34H65N3O5S
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Color White to light yellow
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SMILES
C[C@@]12[C@](C[C@@H](O)[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@]4([H])[C@@H](CC[C@H](C(C)C)OS(=O)(O)=O)C)([H])C[C@@H](NCCCNCCCCN)CC1
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Synonyms
MSI-1256; ENT-01 free acid
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Enzyme Inhib Med Chem
Identification of chemical scaffolds for targeting ubiquitin-specific protease 11 (USP11) through high-throughput virtual screening. [Abstract]2025 Dec;40(1):2518191. PMID: 40588719
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (159.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (4.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (4.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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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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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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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
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Bacterial live/dead nucleic-acid viability staining
The LIVE/DEAD bacterial viability staining method is based on differential permeability of nucleic-acid-binding fluorescent dyes, most commonly SYTO 9 and propidium iodide (PI), which enables discrimination of bacterial populations with intact versus compromised cytoplasmic membranes. SYTO 9 penetrates both intact and damaged bacterial membranes and binds nucleic acids to produce green fluorescence, whereas propidium iodide penetrates only cells with compromised membranes and fluoresces red while also reducing SYTO 9 signal through competitive binding and fluorescence interactions. The resulting fluorescence pattern is interpreted as a proxy for membrane integrity, which is widely used as an indicator of bacterial viability in microscopy, flow cytometry, and spectroscopic platforms. However, mechanistic studies show that SYTO 9 and PI interactions involve displacement and fluorescence resonance energy transfer effects, which can influence signal interpretation depending on dye ratios a
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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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.
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
[1]. Zasloff M, et al. Squalamine as a broad-spectrum systemic antiviral agent with therapeutic potential. Proc Natl Acad Sci U S A. 2011 Sep 20;108(38):15978-83. [Content Brief]
[2]. Márquez-Garbán DC, et al. Squalamine blocks tumor-associated angiogenesis and growth of human breast cancer cells with or without HER-2/neu overexpression. Cancer Lett. 2019 May 1;449:66-75. [Content Brief]
[3]. Djouhri-Bouktab L, et al. Squalamine ointment for Staphylococcus aureus skin decolonization in a mouse model. J Antimicrob Chemother. 2011 Jun;66(6):1306-10. [Content Brief]
[4]. West CL, et al. Squalamine Restores the Function of the Enteric Nervous System in Mouse Models of Parkinson's Disease. J Parkinsons Dis. 2020;10(4):1477-1491. [Content Brief]
[5]. Moore KS, et al. Squalamine: an aminosterol antibiotic from the shark. Proc Natl Acad Sci U S A. 1993 Feb 15;90(4):1354-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.5925 mL | 7.9623 mL | 15.9246 mL | 39.8115 mL |
| 5 mM | 0.3185 mL | 1.5925 mL | 3.1849 mL | 7.9623 mL | |
| 10 mM | 0.1592 mL | 0.7962 mL | 1.5925 mL | 3.9811 mL | |
| 15 mM | 0.1062 mL | 0.5308 mL | 1.0616 mL | 2.6541 mL | |
| 20 mM | 0.0796 mL | 0.3981 mL | 0.7962 mL | 1.9906 mL | |
| 25 mM | 0.0637 mL | 0.3185 mL | 0.6370 mL | 1.5925 mL | |
| 30 mM | 0.0531 mL | 0.2654 mL | 0.5308 mL | 1.3270 mL | |
| 40 mM | 0.0398 mL | 0.1991 mL | 0.3981 mL | 0.9953 mL | |
| 50 mM | 0.0318 mL | 0.1592 mL | 0.3185 mL | 0.7962 mL | |
| 60 mM | 0.0265 mL | 0.1327 mL | 0.2654 mL | 0.6635 mL | |
| 80 mM | 0.0199 mL | 0.0995 mL | 0.1991 mL | 0.4976 mL | |
| 100 mM | 0.0159 mL | 0.0796 mL | 0.1592 mL | 0.3981 mL |
Squalamine Related Classifications
HY-16468 Related Classifications
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