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A cell-permeable phthalimide compound that is reported to inhibit dynamin GTPase activity (IC50 = 17.4 and 63 µM using purified sheep brain dynamin I and recombinant dynamin II, respectively) in a GTP-competitive manner. Shown to block K+-induced SVE (synaptic vesicle endocytosis) of FM4-64 dye into rat brain synaptosomes (IC50 = 12.9 µM), while being ineffective at 30 µM against RME (receptor-mediated endocytosis) of transferrin into human osteosarcoma epithelial U2OS cells, presumably due to poor dynamin II inhibitory potency and/or rapid efflux and/or limited permeability in this cell line.
Dynamin Inhibitor III, Phthaladyn-23 - Calbiochem 分析证书
标题
批号
324412
参考
参考信息概述
Odell, L.R., et al. 2010. J. Med. Chem.53, 5267.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
A cell-permeable phthalimide compound that is reported to inhibit dynamin GTPase activity (IC50 = 17.4 and 63 µM using purified sheep brain dynamin I and recombinant dynamin II, respectively) in a GTP-competitive manner. Shown to block K+-induced SVE (synaptic vesicle endocytosis) of FM4-64 dye into rat brain synaptosomes (IC50 = 12.9 µM), while being ineffective at 30 µM against RME (receptor-mediated endocytosis) of transferrin into human osteosarcoma epithelial U2OS cells, presumably due to poor dynamin II inhibitory potency and/or rapid efflux and/or limited permeability in this cell line.
Form
Light yellow to beige solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₂H₁₂ClN₃O₇
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (7 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.