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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]. | [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.
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| [IC 50]
CDK8: 0.61 nM (IC50); CDK19: 4.28 nM (IC50); GSK3α: 76.67 nM (IC50); GSK3β: 63.06 nM (IC50); STAT5 | [storage]
Store at -20°C | [References]
[1] Akamatsu M, et al. Conversion of antigen-specific effector/memory T cells into Foxp3-expressing Treg cells by inhibition of CDK8/19. Sci Immunol. 2019 Oct 25;4(40). pii: eaaw2707. DOI:10.1126/sciimmunol.aaw2707 |
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cjbscvictory
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www.weikeqi-biotech.com/ |
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