General description

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)