Cayman Cgp 60474, 3-[[4-[2-[(3-Chlorophenyl)Amino]-4-Pyrimidinyl]

CGP 60474 is an inhibitor of cyclin-dependent kinases (CDKs; IC₅₀s = 0.017, 0.08, and 0.05 µM for Cdk1/cyclin B, Cdk2/cyclin A, and Cdk2/cyclin E, respectively). It is selective for these CDKs over Cdk4/cyclin D1 (IC₅₀ = 0.7 µM) and a variety of other kinases, including several PKC isoforms (IC₅₀s = 1.9->100 µM), PKA (IC₅₀ = 160 µM), and FLT1 (IC₅₀ = 1 µM), among others, but does inhibit PKCα and v-Abl (IC₅₀s = 0.25 and 0.4 µM, respectively). It inhibits proliferation of colon, breast, lung, prostate, and ovarian cancer cells (IC₅₀s = 25-84, 21-280, 40 and 68, 17 and 20, and 18-38 nM, respectively). CGP 60474 also reduces LPS-induced IL-6, TNF-α, and RANTES secretion from J774.1 cells in a concentration-dependent manner and inhibits poly(I:C)-induced NF-κB nuclear translocation in the same cells when used at concentrations of 8 and 32 nM. It reduces plasma IL-6 levels and increases survival in a mouse model of LPS-induced endotoxemia when administered at a dose of 10 mg/kg.

WARNING This product is not for human or veterinary use.