Protein kinases are key components in cellular signaling pathways and regulate virtually all aspects of cell life. Deregulation of their activity, caused by genetic mutations or changes in expression levels, has been firmly demonstrated to play a significant role in the pathogenesis of cancer and other diseases. Over the past two decades, protein kinases have become a major class of drug targets. Since the first kinase inhibitor, imatinib, was approved by the FDA in 2001 for the treatment of chronic myeloid leukemia, there have been 82 FDA-approved small-molecule protein kinase inhibitors as of September 2024, predominantly used in cancer therapy.

The human kinome, consisting of 538 protein kinases, makes up about 2% of the human genome and is one of the largest superfamilies of homologous proteins. The FDA-approved small-molecule kinase inhibitors target only approximately 50 of the 538 members of the kinome, indicating significant room for further exploration. Despite the extraordinary success of these kinase inhibitors in the clinic, the kinase drug discovery field is still in its infancy, and challenges remain, including validating novel kinase targets, overcoming drug resistance, attaining exquisite selectivity, expanding applications in non-oncology therapeutic areas (e.g., autoimmune and inflammatory diseases, neurodegenerative disorders, and infectious diseases), and developing efficient compound screening and profiling technologies.

For over 20 years, SignalChem Biotech - now part of Sino Biological - has dependably supported researchers in academia and industry worldwide by offering the world's largest portfolio of highly active kinases, custom enzyme and assay development, and swift compound screening and profiling services. SignalChem Biotech dedication to crafting active kinases is well-documented in more than 2,000 customer publications in high impact journals and is reflected in the support for kinase drug discovery efforts across a wide range of pharmaceutical and biotech clients. Discover SignalChem Biotech’s top-notch recombinant kinases and tailored solutions for your diverse research needs throughout kinase drug discovery.