AS2863619

Catalog No.S8903 Batch:S890301

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Technical Data

Formula

C16H14Cl2N8O
Molecular Weight 405.24 CAS No. 2241300-51-4
Solubility (25°C)* In vitro Water 81 mg/mL (199.88 mM)
DMSO 60 mg/mL (148.06 mM)
Ethanol 4 mg/mL (9.87 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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]
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]

Protocol (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    C57BL/6, BALB/c, NOD, and BALB/c-nu/nu mice

  • Dosages

    30 mg/kg

  • Administration

    Oral gavage

Selleck's AS2863619 has been cited by 1 publication

Enhanced T cell effector activity by targeting the Mediator kinase module [ Science, 2022, 378(6620):eabn5647] PubMed: 36356142

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.