AS2863619

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AS2863619 是一种口服活性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 is an orally active?inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19 (IC50s of 0.61 nM and 4.28 nM, respectively).

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. Western Blot Analysis 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.

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. 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.

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JAK/STAT Signaling

STAT

STAT5|CDK8|CDK19

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2241300-51-4

405.24

C16H14Cl2N8O

>98% (HPLC)

DMSO:245 mg/ml(604.58 mM; Need ultrasonic)

Cl.Cl.Cc1nc2ccc(cc2[nH]1)-n1c(nc2cnccc12)-c1nonc1N

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(-20℃)

With Ice Pack

≥ 2 years