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.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Chircop, M. et al. 2011. Mol. Cancer Ther.10, 1553.
Hill, T.A., et al. 2009. J. Med. Chem.52, 3762.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 408.58. Empirical Formula: C25H36N4O. Quality Level: 100. Assay: ≥. 99% (HPLC). form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: yellow. solubility: DMSO: 100 . mg/mL, clear, yellow. shipped in: ambient. storage temp.: 2-8°C. SMILES string: O: C(NCCCCCCCC)/C(C#N): C/C1: CN(CCCN(C)C)C2: C1C: CC: C2. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51172312
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 324414-10MG
