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.
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。
UNC10112785 is a novel potent inhibitor of CDK8, CDK19, and CDK9 with IC50 at 1.05, 2.67, and 19.9 nM, respectively, causing MYC loss through both transcriptional and posttranslational mechanisms, and suppressing PDAC anchorage-dependent and anchorage-independent growth, inducing the substantial loss of MYC protein in both two-dimensional (2D) and 3D cell cultures.
JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19. JH-XI-10-02 is a potent and selective degrader of CDK8, with an IC50 of 159 nM, based on PROTAC.
JH-XVI-178 is a highly potent and selective CDK8 19 inhibitor with favorable pharmacokinetic attributes, including low clearance and moderate oral bioavailability.