Table of Contents

    InhibiScreen: A Kinase Inhibitor Screening Tool

    Our InhibiScreen Kinase Inhibitor Assay is a validated kinase inhibitor screening tool offering an easy, fast and reliable solution for analyzing basophil activation status via flow cytometry. With the inclusion of two controls, the assay can provide insight into drug potency and therapeutic efficacy of PI3K, BTK and SYK inhibitors in development. Other features include:

    • Results in 30 minutes
    • Reproducible data when samples are acquired at 0, 24 and 96 hours post-staining

    Why Use An Allergy Test to Define Kinase Inhibitor Efficacy?

    Our InhibiScreen Kinase Inhibitor Assay was specifically developed to address the needs of drug development scientists and provides a validated tool for the high throughput assessment of kinase inhibitors. Basophil degranulation and activation are easily measured via flow cytometry by quantifying the expression of cell surface activation markers such as CD63. Allergic responses, autoimmune disorders and oncology are all comprised of signaling pathways that are involved in modifying basophil activation statuses. Several key kinases that are molecular targets in drug discovery are also main components in the basophil activation cascade, such as PI3Kγ and PI3Kδ, SYK, BTK.

    A Validated Kinase Inhibitor Screening Tool to Measure the Efficacy of Kinase Inhibitors in Development

    Whole blood collected in EDTA was treated with increasing doses of the PI3K inhibitor, CAL-101. As the dose increased, CD63 expression decreased, exemplifying the suppression of PI3K-mediated basophil activation.

    These three plot graphs demonstrate how increasing the dose of CAL-101 decreases CD63 expression with the InhibiScreen Kinase Inhibitor tool.

    MFI Signals Remain Stable Up to 96 Hours Post-staining With InhibiScreen

    Whole blood collected in EDTA was treated with increasing doses of the PI3K inhibitor, CAL-101. Following staining, cells were analyzed immediately and aliquots were stored at 2-8˚C and then analyzed at 24 and 96 hours post-staining. MFI values were plotted for CD63+ activated basophils. The IC50 has been determined to be ~200nM using the InhibiScreen Kinase Inhibitor Assay.

    These two charts show a side-by-side comparison of post-staining MFI values using the InhibiScreen Kinase Inhibitor Assay and a competitor's assay.

    Additional Resources

    Download our brochure and application note, or watch our technical video to learn more about the InhibiScreen Kinase Inhibitor Assay.

    Click this thumbnail to download our Kinase Inhibitor Assay brochure.
    InhibiScreen Brochure
    Click this thumbnail preview to download our Inhibiscreen Kinase Inhibitor Assay App Note
    InhibiScreen Application Note