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AS2863619

CAS No. : 2241300-51-4

MCE 国际站：AS2863619

产品活性：AS2863619 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 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 抑制 CDK8/19 可增强 STAT5 的激活，从而激活 Foxp3 基因。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  JAK/STAT Signaling

作用靶点：CDK  |  STAT

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.

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.

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