Potent and selective CDK inhibitor (Kivalues are 1, 2, 3, 46, 171 and 260 nM for CDK4/cyclin D1, CDK1/cyclin B, CDK2/cyclin E, GSK3α, CDK7/cyclin H and GSK3β). Exhibits no effect against a panel of >120 other kinases (Ki> 5,000 nM). Inhibits the prolifera
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Cyclin-dependent kinase 4 inhibitor
Product Description
R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1. A selective inhibitor of cell cycle and transcriptional cyclin dependent kinases including Cdk1, Cdk2, and Cdk4.
1.DePinto W, Chu XJ, Yin X, Smith M, Packman K, Goelzer P, Lovey A, Chen Y, Qian H, Hamid R et al.. (2006) In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials.. Mol Cancer Ther, 5 (11):(2644-58). [PMID:17121911]
Solution Calculators
Molarity Calculator
Determine the necessary mass, volume, or concentration for preparing a solution.
Dilution Calculator
Determine the dilution needed to prepare a stock solution.
C2329033