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Pitstop2 is an amphipathic protein-bound inhibitor of the clathrin terminal domain (IC50=12 μM) with selectivity. Pitstop2 severely interferes with receptor-mediated endocytosis, HIV entry and synaptic vesicle cycling. Pitstop2 has antitumor activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
2 mg | $48 | In Stock | |
5 mg | $80 | In Stock | |
10 mg | $139 | In Stock | |
25 mg | $289 | In Stock | |
50 mg | $455 | In Stock | |
100 mg | $672 | In Stock | |
1 mL x 10 mM (in DMSO) | $100 | In Stock |
Description | Pitstop2 is an amphipathic protein-bound inhibitor of the clathrin terminal domain (IC50=12 μM) with selectivity. Pitstop2 severely interferes with receptor-mediated endocytosis, HIV entry and synaptic vesicle cycling. Pitstop2 has antitumor activity. |
In vitro | METHODS: HeLa cells were pre-incubated with Pitstop2 (10-30 µM) for 15 min, followed by incubation with Alexa568-Tf for 15 min, and transferrin (Tf) uptake was detected by live cell microscopy. RESULTS: HeLa cells efficiently internalized Tf into perinuclear circulating endosomes when exposed to Alexa56-Tf. Preincubation of HeLa cells with Pitstop2 resulted in a dose-dependent inhibition of Tf uptake with IC50 values of 12-15 µM, which was very similar to that measured by in vitro blockade of the function of lattice protein TD. [1] METHODS: Asynchronously growing HeLa cells were treated with Pitstop2 (0.001-100 µM) for 6 h and assayed for mitotic index. RESULTS: Acute treatment of HeLa cells with Pitstop2 for 6 h resulted in a significant increase in mitotic index, suggesting that Pitstop2 activates the SAC. The effect of Pitstop2 on mitotic index was concentration-dependent, and significant at concentrations as low as 0.01 µM. [2] |
Molecular Weight | 473.36 |
Formula | C20H13BrN2O3S2 |
Cas No. | 1419320-73-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 6.88 mg/mL (14.52 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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