AS2863619

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.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

CDK Inhibitors

Specifications & Purity: 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.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

Molecular Formula: C16H14Cl2N8O

Molecular Weight: 405.24

PubChem CID: 139600293

Storage Temperature: Store at -20°C;Argon charged

Shipped in: Ice chest + Ice pads

UPC:

51442716

Weight:

1.06 Ounces

HazmatClass:

Yes

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

A414258-1mg

Country of Origin:

China

CAS:

2241300-51-4

Product Size:

1mg

Harmonized Tariff Code:

2931.90.90