CDK8-IN-11

CDK8-IN-11 is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer.

CDK8-IN-11 (compound 29, 200 nM) shows inhibitory effects against CDK8 by 73.6% [1].CDK8-IN-11 (0-50 μM, 48 h) inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells[1].CDK8-IN-11 (0-4 μM, 48 h) inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells[1].CDK8-IN-11 (0-4 μM, 24 h) suppresses canonical WNT/β-catenin signaling pathways and deregulates β-catenin-mediated transcription in HCT-116 cells[1].CDK8-IN-11 (0.5-2 μM, 48 h) increases the number of cells in the G1 phase in HCT-116 cells[1].CDK8-IN-11 (0-4 μM) reverses Sorafenib resistance of HCT-116 cells[1].

CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) inhibits tumor growth in CT-26 xenograft mice[1].CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) shows no obvious abnormal behavior within 7 days[1].CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10−6 cm/s[1].

References:
[1]. Yao Yao Yan, et al. Design and Synthesis of a 2-Amino-pyridine Derivative as a Potent CDK8 Inhibitor for Anti-colorectal Cancer Therapy. J Med Chem. 2022 Sep 20.