10mM in DMSO pour les flux de travail chromatographiques et analytiques sensibles nécessitant une interférence de ligne de base minimale.
Store at -80°C Expédition Dry ice packs + Cold packs. Consultez le COA spécifique au lot pour les spécifications exactes.
SDS, COA, fiche technique et fiche de spécifications disponibles au téléchargement. COA spécifique au lot accessible via la recherche par numéro de lot.
Cité dans 0 publications à comité de lecture couvrant la chromatographie, la synthèse organique et les réactions de couplage croisé.
AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (T reg ) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC 50 s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19 , which consequently activates the Foxp3 gene
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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. T reg 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice with DNFB-induced contact skin hypersensitivity 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.
IC50& Target:CDK8 0.61 nM (IC 50 ) CDK19 4.28 nM (IC 50 ) GSK3α 76.67 nM (IC 50 ) GSK3β 63.06 nM (IC 50 ) STAT5
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