YJZ5118

YJZ5118 is a potent, selective inhibitor of recombinant CDK12/Cyclin K and CDK13/Cyclin K with IC₅₀ values of 39.5 nM and 26.4 nM, respectively, and over 100-fold selectivity relative to most other CDK family members^[1].
YJZ5118 (0.1 μM; 2 h) acts as an irreversible inhibitor in VCaP prostate cancer cells, maintaining suppression of RNA polymerase II Ser2 phosphorylation, DDR gene expression, and antiproliferative activity after compound washout^[1].
YJZ5118 (5 days) potently inhibits VCaP prostate cancer cell proliferation with an IC₅₀ of 23.7 nM, and shows preferential activity against multiple cancer cell lines including prostate, breast, and Ewing's sarcoma cells, while normal/non-neoplastic cells are less sensitive^[1].
YJZ5118 (20-100 nM; 1-48 h) inhibits RNA polymerase II Ser2 phosphorylation, suppresses transcription of long DDR genes, induces DNA damage, and triggers apoptosis in VCaP prostate cancer cells at concentrations as low as 100 nM^[1].
YJZ5118 (10-100 nM; 24 h) dose-dependently activates the Akt pathway in VCaP prostate cancer cells, and exhibits synergistic antiproliferative effects with multiple Akt inhibitors in 22RV1 prostate cancer cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.