Wiskostatin
Based on 2 publication(s) in Google Scholar
Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization by stabilization of the closed, autoinhibited conformation, thereby preventing Arp2/3 complex activation. Wiskostatin is also a dynamin inhibitor with an IC50 value of 20.7 μM and a potent inhibitor of clathrin-mediated endocytosis with an IC50 value of 6.9 μM. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels. Wiskostatin also induces disassembly of podosomes in a murine monocyte cell line.
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- Purity: 99.87%
- CAS No.: 253449-04-6
- 화학식: C17H18Br2N2O
- 분자량:426.15
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Wiskostatin
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L6 | IC50 |
3657 nM
Compound: 1C
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Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
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[PMID: 27312008] |
Wiskostatin (10-50 μM, 2 h) inhibits Arp2/3-dependent apical biosynthetic traffic and decreases the accumulation of sialylated HA in Madin-Darby canine kidney cells[1].
Wiskostatin (5 μM, 5-15 min) inhibits activation of the WASp biosensor, revealing a reduction in the number of cells displaying podosomes as a function of time in RAW/LR5 cells[4].
Wiskostatin (5 μM, 5 min) inhibits phagocytosis of EIgG by bone marrow-derived macrophage (BMM) and RAW/LR5 cells and decreases phagocytosis in BMM from WASP-deficient mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Madin-Darby canine kidney cells
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Concentration:10-50 μM
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Incubation Time:2 h
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Result:Decreased the accumulation of sialylated HA compared with a mock-treated sample in a dose-dependent manner.
Chemical Information
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CAS No. 253449-04-6
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Appearance Solid
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분자량 426.15
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화학식 C17H18Br2N2O
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Color White to off-white
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SMILES
BrC1=CC=C2C(C3=C(N2CC(CN(C)C)O)C=CC(Br)=C3)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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J Extracell Vesicles
Neuronal Extracellular Vesicles Carrying APOE Downregulate Filament Actin Polymerization Signaling to Inhibit Synapse Formation in Alzheimer's Disease. [Abstract]2026 Mar;15(3):e70248. PMID: 41806350 -
용액&용해도
DMSO : 25 mg/mL (58.66 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
순도&문서
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Data Sheet (280 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Guerriero CJ, et al. N-WASP inhibitor wiskostatin nonselectively perturbs membrane transport by decreasing cellular ATP levels. Am J Physiol Cell Physiol. 2007;292(4):C1562-C1566. [Content Brief]
[2]. Cossar PJ, et al. Wiskostatin and other carbazole scaffolds as off target inhibitors of dynamin I GTPase activity and endocytosis. Eur J Med Chem. 2023 Feb 5;247:115001. [Content Brief]
[3]. Nürnberg A, et al. Pharmacological inhibition of actin assembly to target tumor cell motility. Rev Physiol Biochem Pharmacol. 2014;166:23-42. [Content Brief]
[4]. Dovas A, et al. Regulation of podosome dynamics by WASp phosphorylation: implication in matrix degradation and chemotaxis in macrophages. J Cell Sci. 2009 Nov 1;122(Pt 21):3873-82. [Content Brief]
[5]. Park H, et al. Cdc42 regulates Fc gamma receptor-mediated phagocytosis through the activation and phosphorylation of Wiskott-Aldrich syndrome protein (WASP) and neural-WASP. Mol Biol Cell. 2009 Nov;20(21):4500-8. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3466 mL | 11.7330 mL | 23.4659 mL | 58.6648 mL |
| 5 mM | 0.4693 mL | 2.3466 mL | 4.6932 mL | 11.7330 mL | |
| 10 mM | 0.2347 mL | 1.1733 mL | 2.3466 mL | 5.8665 mL | |
| 15 mM | 0.1564 mL | 0.7822 mL | 1.5644 mL | 3.9110 mL | |
| 20 mM | 0.1173 mL | 0.5866 mL | 1.1733 mL | 2.9332 mL | |
| 25 mM | 0.0939 mL | 0.4693 mL | 0.9386 mL | 2.3466 mL | |
| 30 mM | 0.0782 mL | 0.3911 mL | 0.7822 mL | 1.9555 mL | |
| 40 mM | 0.0587 mL | 0.2933 mL | 0.5866 mL | 1.4666 mL | |
| 50 mM | 0.0469 mL | 0.2347 mL | 0.4693 mL | 1.1733 mL |
Wiskostatin Related Classifications
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