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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $34 | In Stock | In Stock | |
| 5 mg | $80 | In Stock | In Stock | |
| 10 mg | $139 | In Stock | In Stock | |
| 25 mg | $289 | In Stock | In Stock | |
| 50 mg | $455 | In Stock | In Stock | |
| 100 mg | $672 | - | In Stock | |
| 200 mg | $957 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $88 | In Stock | 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 |
| Smiles | S(NC=1S/C(=C\C2=CC=C(Br)C=C2)/C(=O)N1)(=O)(=O)C=3C4=C(C=CC3)C=CC=C4 |
| Relative Density. | 1.60 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 22 mg/mL (46.48 mM), Sonication is recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.23 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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