CDK8-IN-12 is a selective, potent and orally active inhibitor of CDK8 (Ki: 14 nM) and is an anti-cancer agent. CDK8-IN-12 inhibits GSK-3α, GSK-3β and PCK-θ with Ki of 13 nM, 4 nM and 109 nM respectively. CDK8-IN-12 showed anti-proliferative activity against MV4-11 cells.

CDK8-IN-1 is a selective CDK8 inhibitor (IC50: 3 nM).

CDK8-IN-13 is a CDK8 inhibitor (IC50: 51.9 nM) with potent, selective and oral activity. CDK8-IN-13 induces apoptosis and reduces the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 exhibits anti-tumour activity.

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

CDK8-IN-3 is an inhibitor of CDK8.

CDK8-IN-11 hydrochloride is a selective and potent inhibitor of CDK8 (IC50: 46 nM). CDK8-IN-11 hydrochloride inhibits the WNT/β-catenin signalling pathway. CDK8-IN-11 hydrochloride can be used to study colon cancer.

CDK8-IN-4 is an inhibitor of CDK8 (IC50: 0.2 nM).

CDK8-IN-9 (compound 22) is a potent inhibitor of type II CDK8 (IC50: 48.6 nM) and has shown inhibitory effects on tumour growth. CDK8-IN-9 can be used to study colorectal cancer.

CDK8-IN-7 (compound 12) is a potent and selective inhibitor of cyclin-dependent kinase 8 (CDK8) (Kd: 3.5 nM). CDK8-IN-7 has shown potential for AML-cancer research.

CDK8-IN-11 is a potent and selective inhibitor of CDK8, demonstrating an IC50 of 46 nM, and effectively targets the WNT/β-catenin signaling pathway. This compound has potential applications in colon cancer research [1].

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).

CDK8-IN-6 (compound 9) is a potent inhibitor of cyclin-dependent kinase 8 (CDK8) (Kd: 13 nM), CDK8-IN-6 showed potential research value in AML cancers.

CDK8-IN-5 is a potent inhibitor of CDK8, exhibiting an inhibitory concentration (IC 50) of 72 nM. Demonstrating anti-inflammatory properties, it achieves a 43% enhancement rate of IL-10. This compound holds potential for inflammatory bowel disease research.

CDK8-IN-4k is a potent and highly selective CDK8 inhibitor, with no apparent potential for time-dependent CYP3A4 inhibition.

CDK8-IN-10 is a selective and potent inhibitor of cell cycle protein-dependent kinase (CDK8) (IC50: 8.25 nM) that can be used to study cancer.

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.

Senexin C is a novel orally active and specific CDK8/19 inhibitor with potential anticancer activity.Senexin C is more metabolically stable and potent than Senexin B. Senexin C inhibits the growth of MV4-11 leukaemia cells.

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

3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor. In cells expressing analog-sensitive Plk1 alleles, 3MB-PP1 blocks mitotic progression and cell division arise by targeting Plk1. 3MB-PP1 specifically inhibits analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase with IC50 of 2 μM. 3MB-PP1 can be used for the research of cell division and hypha formation of Candida albicans.

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-VIII-49 is an effective and selective inhibitor of CDK8.

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

LL-K8-22 is a potent, selective, and durable dual degrader of CDK8-cyclin C, demonstrating DC50 values of 2.52 and 2.64 μM, respectively. This compound effectively suppresses STAT1 Ser 727 phosphorylation and inhibits carcinogenic transcriptional programs driven by E2F and MYC. LL-K8-22 is specifically utilized in research for triple-negative breast cancer (TNBC) [1].

NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP +/- NU1085 (10 microM) for 72 h.

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.

MSC2530818 is an effective, selective and orally available CDK8 inhibitor (IC50: 2.6 nM).

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

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.

LY2857785 is a type I competitive and reversible ATP kinase inhibitor against CDK7/CDK8/CDK9 (IC50s: 246 nM/16 nM/11 nM).

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.

Fipravirimat is a potent inhibitor of HIV-1 with potential applications in HIV and AIDS research.

Senexin A hydrochloride functions as a selective inhibitor of CDK8/19, with an IC 50 of 280 nM for CDK8, and specifically inhibits p21-induced transcription without affecting other biological effects of p21. Additionally, it suppresses CMV-GFP induction and the stimulatory activity of the consensus NF-κB-dependent promoters [1] [2].

DS96432529 is a potent and orally active bone anabolic agent through CDK8 inhibition.

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

BI-1347 is a potent, selective inhibitor of CDK8/cyclinC (IC50: 1 nM). It shows tumor growth inhibition in an in vivo xenograft model.

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

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.

Wogonin (Vogonin) is a cell-permeable and orally available flavonoid that displays anti-inflammatory and anticancer properties.

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