CDK12/13-IN-3 is a selective inhibitor of cyclin-dependent kinases 12 and 13, demonstrating IC50 values of 107.4 nM and 79.4 nM, respectively. This compound effectively inhibits the phosphorylation of Ser2 on the C-terminal domain of RNA polymerase II, leading to DNA damage and downregulation of DNA damage response gene expression. CDK12/13-IN-3 exhibits notable antiproliferative activity against a variety of cancer cell lines and shows significant antitumor effects in mouse models, supported by favorable pharmacokinetic properties, including an oral bioavailability of 53.6%.
CDK12/13-IN-3 is a selective inhibitor of cyclin-dependent kinases 12 and 13, demonstrating IC50 values of 107.4 nM and 79.4 nM, respectively. This compound effectively inhibits the phosphorylation of Ser2 on the C-terminal domain of RNA polymerase II, leading to DNA damage and downregulation of DNA damage response gene expression. CDK12/13-IN-3 exhibits notable antiproliferative activity against a variety of cancer cell lines and shows significant antitumor effects in mouse models, supported by favorable pharmacokinetic properties, including an oral bioavailability of 53.6%.
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