|Description||R547 is orally bioavailable diaminopyrimidine cyclin-dependent kinase inhibitor (CDKI) with potential antineoplastic activity. CDKI 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. Through CDK inhibition, this agent also reduces phosphorylation of the retinoblastoma (Rb) protein, thus preventing activation of transcription factor E2F and so further suppressing tumor cell proliferation. CDKs are ATP-dependent serine/threonine kinases that are important regulators of cell cycle progression and are frequently overexpressed in tumor cells.|
|Appearance||White to off-white solid|
|Synonyms||RO-4584820; RO4584820; RO 4584820. R 547; R547; R-547|
|Current Developer||F. Hoffmann-La Roche Ltd.|
Dinaciclib, also known as SCH727965, is a potent CDK inhibitor with potential antineoplastic activity. Dinaciclib selectively inhibits cyclin dependent kinases ...
BS-181 HCl is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
CDK9-IN-2 is a novel cyclin-dependent kinase 9(CDK9) inhibitor.
Purvalanol A is a potent CDK inhibitor, which effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src. indicating that the activati...
PHA-767491 is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication.
BS-181 is a highly selective CDK inhibitor for CDK7 with an IC(50) of 21 nmol/L. Testing of other CDKs as well as another 69 kinases showed that BS-181 only inh...
LEE011 succinate hydrate
LEE011 succinate hydrate is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with pot...
BIO (6-bromoindirubin-3'-oxime) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor.