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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: PIM kinases (Proviral Integration of Molony murine leukemia virus), PIM1, PIM2 and PIM3, are a family of serine/threonine protein kinases that play crucial roles in cell survival, proliferation, and drug resistance. PIM kinases are overexpressed in several tumors and promote growth and survival of malignant cells through cell cycle regulation and/or inhibition of apoptosis. PIM1 has two isoforms that differ in length and localization, with the short isoform being found in the nucleus and the longer one in the plasma membrane. This protein is constitutively active, stabilized by phosphorylation. It is normally found in the thymus, spleen, bone marrow, fetal liver, and lymphocytes. It sits at a crosspoint of multiple pathways, being the effector in response to several cytokine activated pathways and acting on several proteins. In T cells, PIM1 enables cells to bypass the TCR (T cell receptor) checkpoint and enhance NFAT (nuclear factor of activated T-cells) activity and IL-2 secretion. High levels of PIM1 can be found in many cancer types, such as hematological disorders and prostate cancer. In triple-negative breast cancer, PIM-1 is a coactivator of Myc, phosphorylates histone H3 leading to stimulation of RNA polymerase II binding, and increased c-Myc driven transcription. The use of PIM1 inhibitors in cancer treatment, as monotherapy, has focused on using ATP competitive or mimetic molecules. The development of new inhibitors to be used in mono- or combinatory therapy will continue to expand the repertoire of tools available in cancer therapy.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ PIM1 Kinase Assay Kit is designed to measure PIM1 (Proviral Integration of Molony murine leukemia virus 1) serine/threonine kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 96-well format, with enough purified PIM1, kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: P11309
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Arrouchi H., et al., 2019 Bioinformation 15(1): 40-45.
Liu Z., et al., 2020 Am J Cancer Res 10(12): 4085-4097.
Jeyapal G. P., et al., 2018 Anticancer Agents Med Chem, 18(8): 1100-1114.
Asati V., et al., 2019 Eur J Med Chem., 172: 95-108.
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