aladdin 阿拉丁 A414258 AS2863619 2241300-51-4 98%

中文名：AS2863619

英文名：AS2863619

纯度：≥98%

货号：A414258

Cas号：2241300-51-4

存储温度：-20°C储存,充氩

运输条件：超低温运输

产品介绍：

Information

AS2863619 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.

Targets

CDK8 (Cell-free assay); CDK19 (Cell-free assay) 0.6099 nM; 4.277 nM

In vitro

AS2863619 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 vivo

AS2863619 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 

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