AS2863619 (C09-0735-674)

InformationAS2863619 AS2863619 is a small-molecule cyclin-dependent kinase CDK8/19 inhibitor with IC50 of 0.6099 nM and 4.277 nM, respectively. AS2863619 is a potent Foxp3 inducer in T conv cells.TargetsCDK8 (Cell-free assay); CDK19 (Cell-free assay) 0.6099 nM; 4.277 nMIn vitroAS2863619 induction of Foxp3 in vitro does not require exogenous TGF-β. AS2863619-induced iTreg cells can be induced in the presence of inflammatory cytokines such as IL-4, IL-6, and IFN-γ, which appear to hamper Foxp3 gene activation via activation of STATs. AS2863619 is able to generate iTreg cells not only from naïve Tconv cells but also from effector/memory Tconv cells. Furthermore, AS2863619 cannot induce Foxp3 in CDK8 and CDK19 double-deficient T cells. AS2863619-induced iTreg cells require TCR and IL-2 stimulation for their generation and are devoid of Treg-type DNA hypomethylation, which is present in nTreg cells and required for stable Treg function.In vivoAS2863619 induces in vivo Foxp3 induction in antigen-activated T cells. In vivo AS2863619-induced Foxp3+ T cells are able to gradually acquire Treg-specific epigenetic alterations, differentiating into functionally stable Foxp3+ pTreg cells having a more nTreg-like gene expression profile.Cell Research(from reference)Cell lines：PBMCs, Human CD4+ T cells, lymph node cells derived from eFox mice Concentrations：1.0 μM Incubation Time：24 h, 0-44 h. Specifications and Purity: 98%. Molecular Formula: C16H14Cl2N8O. Molecular Weight: 405.24. PubChem CID: 139600293.