cdk19

AS2863619 is an orally active inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19 (IC50s of 0.61 nM and 4.28 nM, respectively).

SEL120-34A is a selective and ATP-competitive inhibitor of CDK8 with IC50s of 4.4 nM, 10.4 nM and 1070 nM for CDK8/CycC, CDK19/CycC and CDK9/cycT. SEL120-34A possesses antitumor activity.

SEL120-34A HCl is a selective, orally available and ATP-competitive inhibitor of CDK8(CDK8/CycC and CDK19/CycC with IC50s of 4.4 nM and 10.4 nM , respectively), with antitumor activity.

CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor (IC50: 2.3 nM).

SNX7886 is a potent PROTAC (proteolysis-targeting chimera) that effectively degrades CDK8 and CDK19, achieving 90% degradation of CDK8 and 80% degradation of CDK19 in 293 cells [1].

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.

CCT251545 analog is a potent and selective CDK8/19 inhibitor (IC50: 5.1 nM and 5.6 nM, respectively). Mediator complex-associated kinases CDK8 and CDK19 are involved in the regulation of multiple transcription pathways. CDK8 plays as an oncogene in gastri

CDK8-IN-18, also known as ZINC584617986, is a potent and selective inhibitor of CDK8, also modulating CDK19.

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.

Senexin A is an effective and selective CDK8 inhibitor that also inhibits CDK19 with Kd values of 0.83 microns and 0.31 microns, respectively.

BRD6989 is an analog of the natural product cortistatin A (dCA). Which inhibits CDK8 and upregulates IL-10. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM.

Cortistatin A is a potent and selective mediator-associated kinase CDK8 and its paralogue CDK19 inhibitor.

CDK8/19-IN-1 is a selective and oral bioavailable CDK8/19 dual inhibitor (IC50s: 0.46 nM, 0.99 nM, and 270 nM for CDK8, CDK19, and CDK9).

Senexin B is a potent and selective inhibitor of CDK8/19(CDK8 and CDK19 with Kds of 140 nM and 80 nM).

SNX2-1-108 is a selective CDK8 and CDK19 inhibitor.

CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells).

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.