Description
Cyclin-dependent kinases (Cdks) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. Cdk1/5 Inhibitor is a pyrazolo [3,4-b] quioxaline that inhibits Cdk1/cyclin B and Cdk5/p25 (IC
50s = 600 and 400 nM, respectively). It less potently inhibits GSK3β (IC
50 = 1 μM) and does not block Cdc25 activity. This compound is used to help define the roles of Cdk1 and Cdk5 in various signaling pathways.
Uses
Cyclin-dependent kinases (CDKs) are protein kinases and involved with the regulation of the cell cycle. NSC 693868 is an inhibitor of Cdk1/cyclin B and Cdk5/p25.?Small molecules that target these protein kinases are valuable tools for investigating cellular signaling pathways and are potential therapeutic agents.
Definition
ChEBI: 2H-pyrazolo[4,3-b]quinoxalin-3-amine is a quinoxaline derivative.
Biological Activity
Inhibitor of cyclin-dependent kinases (cdks) and glycogen synthase kinase-3 (GSK-3). IC 50 values are 0.6, 0.4 and 1 μ M for cdk1/cyclin B, cdk5/p25 and GSK-3 respectively.
IC 50
Cdk1/cyclin B: 600 nM (IC
50); Cdk5/p25: 400 nM (IC
50); GSK-3β: 1 μM (IC
50)
References
[1] MIGUEL A. ORTEGA . Pyrazolo[3,4-b]quinoxalines. A new class of cyclin-Dependent kinases inhibitors[J]. Bioorganic & Medicinal Chemistry, 2002, 10 7: Pages 2177-2184. DOI:
10.1016/s0968-0896(02)00069-x[2] SHAOYONG CHEN. Androgen receptor phosphorylation and stabilization in prostate cancer by cyclin-dependent kinase 1.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2006, 103 43: 15969-15974. DOI:
10.1073/pnas.0604193103[3] TRI K NGUYEN Steven G. Dinaciclib (SCH727965) inhibits the unfolded protein response through a CDK1- and 5-dependent mechanism.[J]. Molecular Cancer Therapeutics, 2014: 662-674. DOI:
10.1158/1535-7163.mct-13-0714[4] SUPACHAI TOPANURAK. High NaCl- and urea-induced posttranslational modifications that increase glycerophosphocholine by inhibiting GDPD5 phosphodiesterase.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2013: 7482-7487. DOI:
10.1073/pnas.1305220110
![3-AMINO-1H-PYRAZOLO[3,4-B]QUINOXALINE Structure](https://www.chemicalbook.com/CAS/GIF/40254-90-8.gif)
