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MTOX1094 Sigma-Aldrich

MRP4 Knockout Caco-2 Cells

one vial

  •  NACRES NA.81



Quality Level   200
biological source   human male colorectal tissue (source disease: colon adenocarcinoma)
application(s)   ADME/TOX: suitable
  drug transporter assay: suitable
  permeability assay: suitable
storage temp.   −196°C
Gene Information   human ... ABCC4(10257)


General description

The C2BBe1 cells, a subclone of Caco-2 cells, correspond to ATCC CRL-2102. The MRP4 knockout C2BBe1 cells are adenocarcinoma, epithelial cells from a human caucasian male (aged 72 years) with functional knockout of the ABCC4 (MRP4) efflux transporter.


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

Features and Benefits

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 knockout of the MRP4 gene eliminates the reliance on chemical inhibitors to determine if a compound is an MRP4 substrate
• The vial format enables the MRP4 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

Legal Information

ADME/Tox Cell Lines License

Safety & Documentation

Safety Information

UN 3245 9
WGK Germany 
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable


Certificate of Analysis (COA)

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Protocols & Articles


Caco-2 Intestinal Drug Transporter Models for More Predictive Drug Absorption

Drug-drug interactions are an important area of research as they can affect pharmacokinetics and safety or efficacy of drugs taken concomitantly. Guidance documents from the U.S. Food and Drug Admini...
Keywords: Absorption, Clinical, Gene expression

The Role of Intestinal Efflux Transporters In Drug Absorption

A key aspect for developing a successful drug involves designing the drug so it can be effectively delivered to the intended site of action. The absorption of a drug is a key component to achieving g...
Michael D. Mitchell, Product Manager, Sigma® Life Science and David C. Thompson, R&D Manager, Sigma Life Science
Biofiles Vol. 8, No. 8
Keywords: Absorption, Active transport, Antibiotics, Gastrointestinal, Gene expression, Metabolism, Pharmaceutical


Drug transport assays in a 96-well system: reproducibility and correlation to human absorption

Andrew Arena, Jeanne Phillips, PhD and Mark Blanchard EMD Millipore Corporation, Life Science Division, Danvers, MA
Keywords: Absorption, Active transport, Chromatography, Diffusion, Environmental, Evaporation, High performance liquid chromatography, Mass spectrometry, Metabolism, Pharmaceutical, Scintillation, Size-exclusion chromatography

Peer-Reviewed Papers


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