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KI1322Dynasore10 mg$176

Chemical Characteristic

Product NameDynasore
CAS No.304448-55-3
Molecular Weight 322.32
FormulaC18H14N2O4
Chemical Name2-Naphthalenecarboxylic acid, 3-hydroxy-, 2-[(3,4-dihydroxyphenyl)methylene]hydrazide
Smilesc1c(c(cc2ccccc12)O)C(=O)N/N=C/c1cc(c(cc1)O)O
Chemical Structure

Biological activities

Dynasore is a cell-permeable inhibitor of dynamin. Dynasore interferes with the GTPase activity of dynamin1, dynamin2, and Drp1, the mitochondrial dynamin in vitro. Dynasore inhibits the GTPase activity of full-length dynamin1 or dynamin2 δPRD stimulated by self-association in a dose-dependent manner with an average IC50 of 15 µM. At 80 µM, dynasore also inhibits the enzymatic activity of the mitochondrial dynamin Drp1. Dynasore also elicits a powerful block in the receptor-mediated endocytosis of LDL. Dynasore acts as a potent inhibitor of endocytic pathways known to depend on dynamin by rapidly blocking coated vesicle formation within seconds of dynasore addition.[1] Dynasore binds to serum proteins and loses activity.[2] Dynasore concentration-dependently improves transforming growth factor (TGF)-β1??and TNF-α??nduced PAI-1 protein expression. Dynasore significantly up-regulates PAI-1 protein and its messenger RNA expressions. Dynasore strongly increases JNK phosphorylation.[3] Dynasore rapidly disrupts F-actin formed in brain cytosol in vitro. Dynasore significantly suppresses serum-induced lamellipodia formation in U2OS cell.[4]

Protocols

In vitro: Dynasore is stored at -20 °C or -80 °C in the dark as a 200 mM solution in DMSO under argon.[2]

References

[1] Macia E, et al. Dynasore, a cell-permeable inhibitor of dynamin. Dev Cell. 2006, 10(6): 839-850.
[2] Kirchhausen T, et al. Use of dynasore, the small molecule inhibitor of dynamin, in the regulation of endocytosis. Methods Enzymol. 2008, 438: 77-93.
[3] Chung CL, et al. Dynasore, a dynamin inhibitor, induces PAI-1 expression in MeT-5A human pleural mesothelial cells. Am J Respir Cell Mol Biol. 2009, 40(6): 692-700.
[4] Yamada H, et al. Dynasore, a dynamin inhibitor, suppresses lamellipodia formation and cancer cell invasion by destabilizing actin filaments. Biochem Biophys Res Commun. 2009, 390(4): 1142-1148.

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