Sino Biological provides a wide selection of tools for the study of cyclin-dependent kinases (CDKs), including recombinant proteins, antibodies (rabbit mAbs, mouse mAbs and rabbit pAbs), ELISA kits, and ORF cDNA clones. Cyclin-dependent kinases (CDKs) are a group of protein kinases that are activated by the formation of a complex with a cyclin and are involved in the regulation of the cell cycle. Cyclin-dependent kinases are serine/threonine kinases. Each cyclin associates with one or two CDKs, and most CDKs associate with one or two cyclins.
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Cyclin-dependent kinases (CDKs) are a group of protein kinases that are activated by the formation of a complex with a cyclin and are involved in the regulation of the cell cycle. Cyclin-dependent kinases are serine/threonine kinases that phosphate proteins on serine and threonine amino acid residues. Each cyclin associates with one or two cyclin-dependent kinases, and most cyclin-dependent kinases associate with one or two cyclins. For example, cyclin-dependent kinase 1 (CDK1) is able to form complex either with cyclin A or cyclin B.; whereas cyclin-dependent kinase 2 (CDK2) is associated with Cyclin A and Cyclin B. Formation of cyclin-CDK complex results in activation of the CDK (cyclin-dependent kinase) active site. A cyclin-CDK complex can be regulated by several kinases and phosphatases, including Wee, and CDK-activating kinase (CAK), and Cdc25.
Cyclin-dependent kinases are considered a potential target for anti-cancer medication. Thus development of molecules that can specifically inhibit cyclin-dependent kinases is of great interest. Currently, some CDK inhibitors such as Seliciclib are undergoing clinical trials. A newly discoved CDK inhibitor is Dinaciclib (SCH 727965) that inhibits CDK2, CDK5, CDK1, and CDK9 activity in vitro with IC(50) values of 1, 1, 3, and 4 nmol/L, respectively. Compared with flavopiridol, SCH 727965 exhibits superior activity with an improved therapeutic index, and is less likely to induce apoptosis. Moreover, SCH 727965 induced regression of established solid tumors in a range of mouse models following intermittent scheduling of doses below the maximally tolerated level. The evidence suggests that SCH 727965 is a potent and selective CDK (cyclin-dependent kinase) inhibitor and a novel cytotoxic agent.
It has been suggested that the cyclin D1/ CDK4 complex is a key regulator of the transition through the G1 phase of the cell cycle. In addition, deregulation of the cyclin D /CDK4 pathway has been identified in multiple tumor types. Thus, cyclin-dependent kinase 4 is a genetically validated therapeutic target; hence, selective CDK4 inhibitors are supposed to be anti-cancer agents.