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AS2863619 CDK8/19 Inhibitor

Cat.No.S8903

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 CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 405.24

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 405.24 Formula

C16H14Cl2N8O

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2241300-51-4 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1=NC2=C(N1)C=C(C=C2)N3C4=C(C=NC=C4)N=C3C5=NON=C5N.Cl.Cl

Solubility

In vitro
Batch:

Water : 81 mg/mL

DMSO : 60 mg/mL (148.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
CDK8 [1]
(Cell-free assay)
0.6099 nM
CDK19 [1]
(Cell-free assay)
4.277 nM
In vitro

AS2863619 induction of Foxp3 in vitro does not require exogenous TGF-β. This compound-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. It is able to generate iTreg cells not only from naïve Tconv cells but also from effector/memory Tconv cells. Furthermore, this chemical cannot induce Foxp3 in CDK8 and CDK19 double-deficient T cells. Its-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]
In vivo

AS2863619 induces in vivo Foxp3 induction in antigen-activated T cells. In vivo this compound-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]
References

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