1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. CDK
    STAT
  3. AS2863619

AS2863619 

Cat. No.: HY-126675A
Handling Instructions

AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.

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AS2863619 Chemical Structure

AS2863619 Chemical Structure

CAS No. : 2241300-51-4

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Description

AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene[1].

IC50 & Target[1]

CDK8

0.61 nM (IC50)

CDK19

4.28 nM (IC50)

GSK3α

76.67 nM (IC50)

GSK3β

63.06 nM (IC50)

STAT5

 

In Vitro

AS2863619 (1 μM; 22 hours; mouse CD4+ T cells) treatment suppresses serine phosphorylation of the PSP motif of STAT5b to ~40% while enhancing tyrosine phosphorylation in the C-terminal domain to ~160% of control-treated samples[1].

Western Blot Analysis[1]

Cell Line: Mouse CD4+ T cells
Concentration: 1 μM
Incubation Time: 22 hours
Result: Suppressed serine phosphorylation of the PSP motif of STAT5b to ~40% while enhancing tyrosine phosphorylation in the C-terminal domain to ~160% of control-treated samples.
In Vivo

AS2863619 (30 mg/kg; oral administration; daily; for 2 weeks; mice) treatment after sensitization with 2,4-dinitrofluorobenzene (DNFB) dampens the degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreases ratios of interferon-γ+ (IFN-γ+) cells in a skin contact hypersensitivity model, when compared with vehicle-treated control mice. Treg depletion before the elicitation of the secondary response abolishes AS2863619-induced suppression. KLRG1+ Foxp3+ T cells are specifically increased in DNFB sensitized AS2863619-treated mice[1].

Animal Model: Mice with DNFB-induced contact skin hypersensitivity[1]
Dosage: 30 mg/kg
Administration: Oral administration; daily; for 2 weeks
Result: The degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreased ratios of interferon-γ+ (IFN-γ+) cells.
Molecular Weight

405.24

Formula

C₁₆H₁₄Cl₂N₈O

CAS No.

2241300-51-4

SMILES

NC1=NON=C1C(N2C3=CC=C4N=C(C)NC4=C3)=NC5=C2C=CN=C5.[H]Cl.[H]Cl

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

AS2863619AS 2863619AS-2863619CDKSTATCyclin dependent kinaseInhibitorinhibitorinhibit

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AS2863619
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