To facilitate the in vitro evaluation for PROTAC®s, Creative Biolabs has established a comprehensive series of package assays, from solubility and chemical stability screen to target ubiquitination and degradation. Amongst, cell cytotoxicity test assay is one of the most experienced services in Creative Biolabs.
PROTAC® can simultaneously recognize target protein and specific E3 ligase which will result in a ternary complex formation. Upon ternary complex formation, E3 ligase will degrade target proteins via proteasome machinery. After target protein degradation, PROTAC® is released and continues the degradation process. This reusable characteristic of PROTAC® contributes to the low toxicity to cells. In addition, PROTAC® only suppresses target protein because of high specificity. Even though, PROTAC® treatment still has toxicity to cells as a foreign small molecule. Thus, evaluating cell cytotoxicity can help us to choose the optimal PROTAC®s with lowest cytotoxicity for further research.
Cytotoxicity assays are normally based on assessing damage to cellular membranes or cell viability or cell apoptosis or cell proliferation. Creative Biolabs has explored a variety of assays for your flexible choice to best fit your projects. We are expertise in conducting the following cytotoxicity assays to evaluate the cytotoxicity caused by PROTAC®s (see Fig.1).
Fig.1 Schematic diagram of cell cytotoxicity assays.
These assays measure the activity of specific enzymes that leak into the extracellular medium occurred after cell membrane damage. Creative Biolabs is capable of offering lactate dehydrogenase (LDH) assay and adenylate kinase (AK) assay to our clients.
These assays utilize membrane impermeable fluorescent dyes to stain the cells with damaged cell membranes. Creative Biolabs provides our clients with the dyes including propidium iodide, ethidium homodimer-1, trypan blue, and 7-AAD.
Amine-reactive dyes can react with intracellular amines once the cell membrane is damaged. However, they have weak binding to cell surface amines of viable cells. If you are interested in this assay, please contact Creative Biolabs.
Creative Biolabs also offers dye combined assays to monitor the live and dead cells together.
These assays are to measure viable cells based on specific dyes or cellular activities. Creative Biolabs offers esterase-cleaved dye, mitochondrial membrane potential-dependent dyes, tetrazolium, resazurin, ATP and ADP assays. In addition, the metabolism assays to measure glycolytic flux and oxygen consumption are also available in Creative Biolabs.
These assays are to measure the biomarkers present in different type of dead cells. Creative Biolabs offers Annexin V, TUNEL and caspase assays.
These assays monitor cell growth via detecting cell divisions or cell cycle states. Creative Biolabs is here to provide dye dilution assay, BrdU/EdU, and DNA staining dyes to you.
With years of exploration in PROTAC® field, Creative Biolabs has established a comprehensive set of package services which involve a variety of assays. We will try our best to fulfill all requirements of our clients to evaluate PROTAC®s and facilitate your projects. We are committed to making efforts for a healthier world. Please contact us for more information and a detailed quote.
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