cdk8

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-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.

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.

AS2863619 is an oral inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19. Inhibition of CDK8 19 can enhance the activation of STAT5, thereby activating the Foxp3 gene. It can convert antigen-specific effector memory T cells into Foxp3+ regulatory T cells to study various immune diseases.

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

CDK8 19-IN-51 is an orally active and highly effective dual inhibitor of CDK8 and CDK19, with anticancer activity. Its IC50 values for CDK8 and CDK19 are 5.1 nM and 5.6 nM, respectively. It is used in studies of colorectal and gastric cancers.

CDK8-IN-14 (compound 12) effectively inhibits CDK8, demonstrating an IC50 of 39.2 nM, and exhibits potent anti-AML cell proliferation effects, with a GC50 value of 0.02±0.01μM in MOLM-13 cells and 0.03±0.01μM in MV4-11 cells [1].

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

CDK8-IN-15 (Compound 46) is a potent inhibitor of CDK8, exhibiting an IC50 value of 57 nM. This compound enhances the thermal stability of CDK8 and inhibits NF-κB, while selectively targeting the CDK family and tyrosine kinases. Additionally, it actively counteracts TNF-α-induced psoriasis in vitro and boosts the expression of Foxp3 and IL-10, potentially diminishing inflammatory responses and showing promise for research into psoriasis treatments.

CDK8-IN-3 [CDK8-IN-3] is a potent and selective inhibitor of CDK8.

CDK8-IN-11 hydrochloride is a selective and potent inhibitor of CDK8 (IC50: 46 nM) that inhibits the WNT β-catenin signaling pathway and can be utilized for studying colon cancer.

CDK8 19-IN-3 (compound 3-7) is a potent and selective inhibitor of CDK8 and CDK19. It can increase IL-10 levels and has potential for research in inflammatory bowel disease (IBD).

CDK8-IN-4, an inhibitor of CDK8, has an IC50 value of 0.2 nM.

CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor (IC50: 48.6 nM) with demonstrated inhibitory effects on tumor growth, making it a valuable tool for studying colorectal cancer.

CDK8-IN-17 (Compound WS-2) is a CDK8 inhibitor with an IC50 value of 9 nM, which may be utilized in cancer research.

CDK8-IN-11 is a selective and potent CDK8 inhibitor that shows antiproliferative activity in colon cancer cell lines, inhibiting WNT β-catenin activation and TCF family transcriptional activity, inducing G1-phase arrest in HCT-116 cells, useful for colon cancer research.

CDK8 19-IN-2 (compound 12) is a potent inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), exhibiting IC 50 values of 2.08 nM and 2.49 nM, respectively. This orally active compound is applicable in the research of acute myeloid leukemia (AML), breast cancer, and lymphoma.

CDK8 19-IN-1 is a selective, orally bioavailable dual inhibitor of CDK8 and CDK19, with IC50 values of 0.46 nM for CDK8, 0.99 nM for CDK19, and 270 nM for [CDK9].

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

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

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

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

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.

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.