Pitstop 2

SKU: orb1305236

Description

Pitstop 2 is a selective, amphipathic small molecule inhibitor of the clathrin terminal domain (IC50=12 µM). It potently blocks clathrin-mediated processes including receptor endocytosis, viral entry, and synaptic vesicle recycling, and exhibits antitumor activity in research models.

Research Area

Cell Biology

Key Properties

• CAS Number: 1419320-73-2
• MW: 473.36
• Purity: >99.99% (May vary between batches)
• Formula: C₂₀H₁₃BrN₂O₃S₂
• 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
• Target: Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.23 mM);DMSO:22 mg/mL (46.48 mM)

Bioactivity

• 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. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CME, clathrin, clathrin-mediated, cancer, Apoptosis, endocytosis, Inhibitor, inhibit, Pitstop 2, Pitstop2, Pitstop-2

Compound Identifiers

PubChem CID

137254289