A cell-permeable, allosteric Dynamin inhibitor (IC50=6.9uM and 14uM for full length Dynamin I and Dynamin II GTPase activity, respectively, in vitro). 10uM 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 - 37uM). It was further shown to be 6-fold more active (IC50=5.0uM) than dynamin mediated receptor mediated endocytosis (RME) in U2OS cells, and 15-fold more active (IC50=1.3uM) than Dynasore in another Dynamin I GTPase activity assay.
Formula:C25H36N4O
Solubility:DMSO
Molecular Weight:408.6
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
