cdk-8-in-1

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

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

CDK8-IN-19 (Compound 3d) is a CDK8 inhibitor with an IC50 of 25.08 nM. It exhibits broad-spectrum anticancer activity, showing effectiveness against leukemia, melanoma, and breast cancer, while demonstrating no significant cytotoxicity to normal Vero cells (mean IC50 values are 2.87, 3.65, 3.79, and 45.48 μM, respectively).

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-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-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.

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

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.

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-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-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.

CDK8/19-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].

CDK2-IN-18 (compound 8q) serves as a powerful inhibitor of CDK 2/E and CDK 4/D1, showing IC50 values of 8 nM and 46 nM, respectively. It effectively inhibits tumor cell proliferation [1].