CDK2/5/9 Inhibitor CYC065
An orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9), with potential antineoplastic and chemoprotective activities. Upon oral administration, CYC065 selectively binds to and inhibits the activity of CDK2, 5 and 9, which leads to inhibition of CDK2, 5 and 9-dependent cellular pathways, downregulation of genes involved in the pro-survival pathway, prevention of the activation of DNA double-strand break repair pathways, and induction of both cell cycle arrest and apoptosis. This inhibits the proliferation of CDK2/5/9-overexpressing tumor cells. In addition, CYC065 protects hematopoietic stem and progenitor cells (HSPCs), prevents myelosuppression, and preserves the function of the bone marrow. CDKs are serine/threonine kinases involved in the regulation of the cell cycle and may be overexpressed in certain cancer cell types; they play key roles in tumor cell proliferation, the regulation of transcription, and DNA damage repair. [ ]
Term info
CDK2/5/9 Inhibitor CYC065
- CDK2/5/9 Inhibitor CYC065
- CYC065
- Cyclin Dependent Kinase Inhibitor 2/5/9 CYC065
NCIT_C116978, NCIT_C128784, NCIT_C116977, NCIT_C157711, NCIT_C157712
CTRP
CDK2/5/9 Inhibitor CYC065
http://purl.obolibrary.org/obo/NCIT_C17767
CL498266
775991
775991
CDK2/5/9 Inhibitor CYC065
Pharmacologic Substance, Organic Chemical
C123902
Term relations
- Antineoplastic Enzyme Inhibitor
- Cyclin-Dependent Kinase Inhibitor
- Chemical_Or_Drug_Has_Mechanism_Of_Action some Enzyme Inhibition
- Chemical_Or_Drug_Has_Physiologic_Effect some Positive Regulation of Apoptosis
- Chemical_Or_Drug_Affects_Gene_Product some Cyclin-Dependent Kinase
- Chemical_Or_Drug_Has_Physiologic_Effect some Negative Regulation of Cell Cycle