MC180295 is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs, such as CDK1-Cyclin B (IC50, 138 nM), CDK2-Cyclin A (IC50, 233 nM), CDK2-Cyclin E (IC50, 367 nM), CDK3-Cyclin E (IC50, 399 nM), CDK4-Cyclin D (IC50, 112 nM), CDK5-P35 (IC50, 159 nM), CDK5-P25 (IC50, 186 nM), CDK6-Cyclin D3 (IC50, 712 nM), and CDK7-CycH/MAT1 (IC50, 555 nM). MC180295 also inhibits GSK-3α and GSK-3β.
MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation.
MC180295 (0.1 μM) inhibits the proliferation in cancer cells.