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AT7519

AT7519 is a potent inhibitor of several cyclin-dependent kinases (CDKs) that showed potent antiproliferative activity (40-940 nmol/L) in a panel of human tumor cell lines. Short-term treatments inhibited phosphorylation of the transcriptional marker RNA polymerase II and caused downregulation of the antiapoptotic protein Mcl-1, without affecting the abundance of XIAP or Bcl-2. The reduced abundance of the Mcl-1 protein level was linked to an increase in cleaved poly(ADP-ribose) polymerase. The mechanism of action was shown to be consistent with the inhibition of CDK1, CDK2 and CDK9 in tumor cell lines.

catalogue number: A012
CAS: 844442-38-2
MW: 382.24 g/mol

References
J Med Chem. 2008 Aug 28;51(16):4986-99. PMID: 18656911
Mol Cancer Ther. 2009 Feb;8(2):324-32. PMID: 19174555
Oncogene. 2010 Apr 22;29(16):2325-36. PMID: 20101221
PDB Structure of its co-crystal with CDK2: 2VTQ