CDK Inhibitor R547
An orally bioavailable diaminopyrimidine compound and a cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. CDKs are ATP-dependent serine/threonine kinases that are important regulators of cell cycle progression and are frequently overexpressed in cancerous cells. R547 selectively binds to and inhibits CDKs, especially CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1. The inhibition of CDKs results in cell cycle arrest, inhibition of tumor cell proliferation, and induction of apoptosis. By inhibiting CDK activity, R547 also reduces phosphorylation of the retinoblastoma (Rb) protein, thereby preventing activation of transcription factor E2F and leading to further suppression of tumor cell proliferation. [ ]
Term info
CDK Inhibitor R547
- CDK Inhibitor R547
- Cyclin Dependent Kinase Inhibitor R547
- Cyclin-Dependent Kinase Inhibitor R547
- R 547
- R-547
- R547
- RO 4584820
- RO-4584820
- RO4584820
NCIT_C63923, NCIT_C128784, NCIT_C157711, NCIT_C157712
741713-40-6
T61871RKRI
http://purl.obolibrary.org/obo/NCIT_C17767
R547
529189
529189
CDK Inhibitor R547
Pharmacologic Substance, Organic Chemical
C1832011
C64544
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_Has_Physiologic_Effect some Protein Phosphorylation Inhibition
- Chemical_Or_Drug_Has_Physiologic_Effect some Negative Regulation of G1 Phase
- Chemical_Or_Drug_Affects_Gene_Product some Cyclin-Dependent Kinase
- Chemical_Or_Drug_Has_Physiologic_Effect some Negative Regulation of G2 to M Transition