Darovasertib

Darovasertib (CAS No.: 1874276-76-2) is a synthetic small-molecule selective inhibitor of protein kinase C (PKC), also known as LXS196 or IDE-196, designed for use in experimental research and drug discovery settings involving kinase signal transduction and tumor biology; it exhibits the strongest inhibitory activity against PKCα and PKCθ within the PKC family, while showing markedly reduced activity against secondary kinases such as GSK3β, thereby helping to specifically interfere with diacylglycerol-dependent PKC signaling pathways and their downstream phosphorylation cascades at the cellular and molecular levels, and further enabling analysis of key nodes related to cell cycle control and survival; in vitro, darovasertib typically demonstrates nanomolar potency against major PKC isoforms in enzymatic assays, and shows proliferation inhibition ranging from low nanomolar to low micromolar levels in sensitive cell models dependent on PKC pathways, such as uveal melanoma and B-cell lymphoma cell lines, whereas certain cutaneous melanoma cells show limited response even at higher micromolar levels, reflecting pathway selectivity and context dependence; based on these characteristics, researchers commonly use it for target validation, pathway mapping, combination screening, and mechanistic “rescue” experiments, as well as the development and optimization of cellular and preclinical models; the dosage and exposure regimen in specific experiments should be conditionally optimized according to the experimental purpose, assay platform, time course, and biomarker readouts; this product is intended solely for laboratory research such as molecular and cell biology and for the discovery and characterization of PKC-dependent mechanisms, and is strictly prohibited for any use related to human applications.