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
- UPC:
- 12141903
- Condition:
- New
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- A414258-25mg
- CAS:
- 2241300-51-4
- Product Size:
- 25mg
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