Senexin A hydrochloride是一种专门针对CDK8 19(IC50为280 nM,针对CDK8)的抑制剂,同时针对p21转录活性下游展现抑制作用。该化合物特异性抑制由p21诱导的转录活性,而不干扰p21的其他生物功能。此外,Senexin A hydrochloride能够抑制CMV-GFP引发的活性及p21激活的、具NF-κB依赖性启动子的表达。
AS2863619 free base enables the conversion of antigen-specific effector memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor (IC50s: 0.61 nM and 4.28 nM). STAT5 activation enhanced by AS2863619 free base inhibition of CDK8 19, which consequently activates the Foxp3 gene.