The C2BBe1 cells, a subclone of Caco-2 cells, correspond to ATCC CRL-2102. The MDR1 and MRP2 knockout C2BBe1 cells are adenocarcinoma, epithelial cells from a human caucasian male (aged 72 years) with functional double knockout of the ABCB1 and ABCC2 (MDR1/MRP2) efflux transporters.

The following posters and articles demonstrate how Caco-2 cells can be used for cell based assays:

Transporter Function in Caco-2 Cells with Targeted P-Glycoprotein, MRP2 and BCRP Gene Knockout Using Zinc Finger Nucleases

Comparison of Function and Relative Transporter Protein Concentrations in Caco-2 Cells with Single and Double Knockouts of the ABCB1, ABCG2, and ABCC2 Genes

Caco-2 Transporter Knockout Cell Based Assays

The Caco-2 subclone C2BBe1 cells are ideal for transporter analysis as they express multiple transporters, are human derived, and grow in a homogenous monolayer that forms tight junctions necessary for efflux ratio analysis. Other benefits include:

• A functional double knockout of the MDR1 gene and MRP2 gene eliminates the reliance on chemical inhibitors to determine if a compound is an BCRP substrate
• The vial format enables the MDR1 and MRP2 knockout cells to be included in standard drug transporter protocols
• Human assay with no interference from animal inhibitors
• Overcome the limitations of RNAi and knockdown cell lines that arise from remaining transporter functionality

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