Atuveciclib

Atuveciclib (CAS No.: 1414943-88-6) is a synthetic small molecule classified as a cyclin-dependent kinase research tool compound, suitable for studies of kinase signaling and transcriptional regulation; as a potent and highly selective P?TEFb/CDK9 inhibitor, it acts on the complex composed of CDK9 and Cyclin T to modulate regulatory phosphorylation events required for RNA polymerase II pause release and productive elongation. In biochemical assays, its IC50 against CDK9/CycT1 is approximately 13 nM, and it shows approximately 100-fold selectivity over CDK2; in addition, it also displays nanomolar inhibitory activity against GSK3α and GSK3β (approximately 45 nM and 87 nM). These properties make it useful for dissecting CDK9-dependent pathways and their downstream gene expression programs; in vitro activity is typically observed in the nanomolar to low micromolar range, depending on the assay format and protein complex composition. In cellular models and animal-derived nonclinical models, it is commonly used for mechanism-of-action studies, target validation, pathway dependency assessment, and as a reference control in screening workflows; the concentrations or doses used in experiments are generally determined according to the specific experimental design and research objectives. A racemate of Atuveciclib has also been reported for comparative studies. For laboratory research use only, not for human ingestion, medical use, or any other non-research applications.