Product Description
ABL(E255K) is a key clinically relevant mutation of ABL1, a non‑receptor tyrosine kinase that plays essential roles in cell proliferation, differentiation, adhesion, and apoptosis. ABL1 is best known for its fusion with BCR to form the BCR‑ABL1 oncoprotein, which serves as the primary driver of chronic myeloid leukemia (CML) and a subset of acute lymphoblastic leukemia (ALL). The E255K mutation resides in the ATP‑binding P‑loop of the ABL1 kinase domain and confers resistance to ATP‑competitive inhibitors, most notably imatinib, by destabilizing inhibitor binding while preserving or enhancing kinase activity. This mutation sustains aberrant downstream signaling through pathways such as STAT5, MAPK, and PI3K/AKT, promoting uncontrolled cell survival and proliferation. It frequently leads to cross‑resistance to multiple first‑ and second‑generation tyrosine kinase inhibitors, making it a critical target for next‑generation inhibitors (e.g., ponatinib) and combination strategies in precision oncology and drug resistance research.
Screeningbio’s ABL(E255K) Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying ABL(E255K) kinase activity and evaluating the potency of tyrosine kinase inhibitors (TKIs).
This kit utilizes the ADP-Glo Kinase Assay platform, a luminescent technology that measures the amount of ADP produced during the kinase reaction.
The assay is performed in two distinct steps:
Kinase Reaction: ABL(E255K) catalyzes the transfer of a phosphate group from ATP to a specific substrate, resulting in the production of phosphorylated substrate and ADP.
ADP-Glo™ Reagent Addition: After the kinase reaction, the ADP-Glo™ Reagent is added to terminate the reaction and deplete any remaining unreacted ATP.
Kinase Detection: The Kinase Detection Reagent is added to simultaneously convert the produced ADP back into ATP, which is then used by luciferase to generate a luminescent signal.
The light intensity produced is directly proportional to the ADP concentration and, consequently, to the enzymatic activity of the ABL(E255K) kinase.
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