AS2863619 free base 可以将抗原特异性效应子/记忆 T 细胞转换为 Foxp3⁺ 调节性 T (T_reg) 细胞，以研究各种免疫疾病。AS2863619 free base 是一种有效的口服的细胞周期蛋白依赖性激酶 8 (CDK8) 和 CDK19 抑制剂，IC₅₀ 分别为 0.61 nM 和 4.28 nM。AS2863619 free base 抑制 CDK8/19 可增强 STAT5 的激活，从而激活 Foxp3 基因。

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.

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CDK8 0.61 nM (IC50) CDK19 4.28 nM (IC

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. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis-tbl">

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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[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.

In Vitro: DMSO : 250 mg/mL (752.29 mM; Need ultrasonic)配制储备液