Home Cell Cycle CDK inhibitor AS2863619 For research use only.

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 Tconv cells.

AS2863619 Chemical Structure

AS2863619 Chemical Structure

CAS: 2241300-51-4

Selleck's AS2863619 has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.89%
99.89

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Biological Activity

Description 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 Tconv cells.
Targets
CDK8 [1]
(Cell-free assay)		 CDK19 [1]
(Cell-free assay)
0.6099 nM 4.277 nM
In vitro
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.[1]
Cell Research 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
Method

2 × 105 CD4+ DO11.10 T cells are plated with 4 × 104 T cell–depleted splenocytes in the presence of 5 μM OVA peptide. AS2863619 is used at 1.0 μM, except where noted.
In Vivo
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.[1]
Animal Research Animal Models C57BL/6, BALB/c, NOD, and BALB/c-nu/nu mice
Dosages 30 mg/kg
Administration Oral gavage

Chemical lnformation & Solubility

Molecular Weight 405.24 Formula

C16H14Cl2N8O
CAS No. 2241300-51-4 SDF --
Smiles CC1=NC2=C(N1)C=C(C=C2)N3C4=C(C=NC=C4)N=C3C5=NON=C5N.Cl.Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Water : 81 mg/mL

DMSO : 60 mg/mL ( (148.06 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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