CCT251545 - 99%, high purity , CAS No.1661839-45-7, Inhibitor of cyclin dependent kinase 19;Inhibitor of cyclin dependent kinase 8

Item Number

C413899

• Specifications & Purity: Moligand™, ≥99%
• Biochemical and Physiological Mechanisms: CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
• Storage Temp: Store at -20°C,Argon charged
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of cyclin dependent kinase 19;Inhibitor of cyclin dependent kinase 8

Product Description

Information

CCT251545 CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.

Targets

CDK8 ; CDK19 ; Wnt (in 7dF3 cells) ; 5 nM

In vitro

The suppression of the WNT pathway activity by CCT251545 is not unique to a specific cell line, is independent of exogenous WNT pathway stimulation, does not result from destabilization of TCF1 or TCF4, and is not due to interference with the luciferase-based reporter readout. CCT251545 also demonstrates a lack of transporter-mediated efflux and a lack of activity across broad in vitro panels of enzyme, receptor, and ion channel targets.

In vivo

CCT251545 is a potent small-molecule inhibitor of WNT signaling with good oral pharmacokinetics. We demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing.

Cell Research(from reference)

Cell lines：7dF3 cells, HEK293 cells, SW480, LS174T, COLO205 human colorectal cancer cells 

Concentrations：9.1 μM - 0.068 nM 

Incubation Time：2 h, 6 h