253449-04-6
Chemical Structure
Wiskostatin
- CAS. Nr.: 253449-04-6
- Formula:C17H18Br2N2O
- Molecular Weight:426.15
IUPAC Name: 1-(3,6-dibromo-9H-carbazol-9-yl)-3-(dimethylamino)propan-2-ol
InChIKey: XUBJEDZHBUPBKL-UHFFFAOYSA-N
SMILES: BrC1=CC=C2C(C3=C(N2CC(CN(C)C)O)C=CC(Br)=C3)=C1
Biological Activity: 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[1][2][3][4][5].
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Wiskostatin | 99.87% | 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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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]
