Portal Powers all your Macrocycle Workflows

• Primary hit discovery or cell-based screening of otherwise impermeable compounds
• Hit validation, SAR/lead optimization, and target-engagement studies
• Translation into more complex biological systems, like your cells!

Dose-Dependent Intracellular Delivery in HeLa Cells.

Intracellular delivery of macrocycles into HeLa cells was achieved with efficiency. Following delivery, the percentage of FITC-positive live cells showed a strong, clear, dose dependent increase. Untreated cells (0 mg/ml) exhibited 0% delivery, treated cells achieved approximately 50% delivery efficiency at lowest active dose of 0.025 mg/ml. This efficiency scaled up ~80% at 0.05 mg/ml, and achieved near-total intracellular delivery–approximtely 90% to 100% efficiency–at the peak macrocycle concentrations of 0.1 mg/ml and 0.2 mg/ml. These results demonstrate the platform’s ability to drive cargo uptake at scale while preserving overall cell integrity, enabling typical dose-response curve generation in drug discovery experiments.

Sustained Viability in HeLa Cells Across Escalating Macrocycle Doses

Portal’s platform technology enables macrocycle delivery without compromising cell health. HeLa cell viability remained stable at ~80% across increasing macrocycle concentrations up to 0.2 mg/ml. This consistent viability across a wide dose range highlights exceptionally low cytotoxicity of Portal’s delivery method.

Delivery of Macrocycle to HEK293 cells

HEK293 cells treated with FITC-labeled macrocycles utilizing Portal’s delivery technology. Fluorescence microscopy provides visual evidence of successful macrocycle delivery, showing robust intracellular accumulation of FITC-labeled macrocycles in boosted HEK293 cells.

Macrocycle Delivery and Maintained Viability  in HEK293 Cells

Flow cytometry demonstrates that the Portal delivery platform achieves exceptional efficiency while preserving overall HEK293 cell health. Quantitative analysis revealed ~80% successful uptake of FITC-labeled macrocycles by boosted cells. Crucially, this effective intracellular delivery was accomplished while maintaining strong overall viability at ~80%. These metrics demonstrate the platform's ability to balance highly efficient cargo delivery with the preservation of a robust live cell population.