CDK7/9-IN-1 is a specific inhibitor of cyclin-dependent kinases 7/9 (CDK7/9). It specifically targets CDK7, while also displaying inhibitory activity against CDK9. CDK7/9-IN-1 demonstrates excellent inhibitory potency against CDK7, with IC50 values of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. Furthermore, CDK7/9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. Its application in cancer research makes it valuable for such investigations.

CDK7:5.74-65.6 nM (IC50), CDK9:2.14 μM (IC50)

CDK7/9-IN-1 (example 8; 0.001-20 μM; 4 h) inhibits CDK7 with an relative IC 50 of 0.0262 μM for phospho-carboxyl terminal domain (Rbp2) (Ser5) in HCT116 cells[1]. CDK7/9-IN-1 (0.001-20 μM; 4 h) inhibits CDK9 with an IC 50 of 2.59 μM for phospho-carboxyl terminal domain (Rbp2) (Ser2) in HCT116 cells[1]. CDK7/9-IN-1 (0.001-20 μM; 4 h) inhibits cMyc with an relative IC 50 of 0.0138 μM in HCT116 cells[1]. CDK7/9-IN-1 (20 μΜ, 2 μΜ, and 0.2 μΜ; 1 h) shows excellent selectivity against the 468 protein kinases panel. CDK7/9-IN-1 shows approximately 96% inhibition against CDK7[1].