MC180295

MC180295 ((rel)-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. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect^[1]. IC50 & Target: IC50: 5 nM (CDK9-Cyclin T1), 138 nM (CDK1-Cyclin B), 233 nM (CDK2-Cyclin A), 367 nM (CDK2-Cyclin E), 399 nM (CDK3-Cyclin E), 112 nM (CDK4-Cyclin D), 159 nM (CDK5-P35), 186 nM (CDK5-P25), 712 nM (CDK6-Cyclin D3), 555 nM (CDK7-CycH/MAT1)^[1] In Vitro: 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^[1].
MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation^[1].
MC180295 (0.1 μM) inhibits the proliferation in cancer cells^[1]. In Vivo: MC180295 (20 mg/kg, i.p., qod) inhibits significant anti-tumor activity in mice bearing SW48 cells, shows no inhibitory activity against human T cell growth in vivo^[1].