Dynamin Inhibitor V, 34-2

A cell-permeable, allosteric Dynamin inhibitor (IC₅₀ = 6.9 µM and 14 µM for full length Dynamin I and Dynamin II GTPase activity, respectively, in vitro). 10 µM of this compound results in cytokinesis failure at the abscission stage in HeLa cultures, with 82% of cells that enter into mitosis becoming multinucleated, and with 97% resulting in cell death. However, it displays a much reduced effect in NIH3T3 cells at the same concentration. It elicits a dose-dependent reduction in cell growth against SMA-560, SJ-G2, SW480, MCF-7 and A2780 cultures, as being the most sensitive among a panel of other cancer cell lines (GI₅₀ = 4.0–37 µM). It was further shown to be 6-fold more active (IC₅₀ = 5.0 µM) than dynamin mediated receptor mediated endocytosis (RME) in U2OS cells, and 15-fold more active (IC₅₀ = 1.3 µM) than Dynasore (Cat. No. 324410) in another Dynamin I GTPase activity assay.

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Chircop, M. et al. 2011. Mol. Cancer Ther.10, 1553.
Hill, T.A., et al. 2009. J. Med. Chem.52, 3762.

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