CDK7/9-IN-1

CDK7/9-IN-1 is a cyclin-dependent kinases 7/9 (CDK7/9) inhibitor. CDK7/9-IN-1 selectively inhibits CDK7 over CDK9. CDK7/9-IN-1 inhibits CDK7 with IC50s of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. CDK7/9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. CDK7/9-IN-1 can be used for the research of cancer[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

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 IC50 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 IC50 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 IC50 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].

[1]. Maria Carmen FERNANDEZ FIGUEROA, et al. Compounds useful for inhibiting cdk7. WO2021242602 A1.