cdk9-in-10

CDK9-IN-10 is a potent inhibitor of CDK9 and serves as the ligand for the PROTAC CDK9 degrader-2.

CDK9-IN-40 is an inhibitor of CDK2 (Cyclin-dependent kinase 2). It effectively inhibits CDK2/Cyclin E1, with an IC50 of ≤ 10 nM.

Olomoucine II is a potent cyclin-dependent kinase inhibitor with IC50 values of 7.6, 0.1, 19.8, 0.45, and 0.06 μM for CDK1, CDK2, CDK4, CDK7, and CDK9, respectively. Olomoucine II demonstrates high selectivity over numerous other kinases while retaining measurable activity against ERK2 and ABCB1, allowing it to modulate multidrug resistance pathways. Olomoucine II suppresses proliferation across cancer cell lines regardless of p53 status and exhibits synergistic action with daunorubicin in ABCB1-expressing HCT-8 cells.Olomoucine II additionally inhibits replication of HSV-1, HSV-2, vaccinia virus, adenovirus 4, and human CMV, making Olomoucine II an important antiviral and anticancer research tool.

CDK12-IN-2 (CDK12 inhibitor 2) is an effective and selective inhibitor of CDK12 with an IC50 of 52 nM, >100 μM, >10 μM and 16 μM for CDK12, CDK2, CDK7, and CDK9. CDK12-IN-2 can be used in studies about the function of CDK12.

EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR (IC50:191.08 nM), HER2 (IC50:132.65 nM), and CDK9 (IC50:113.98 nM), demonstrating significant anti-tumor effects.

CDK9/10/GSK3β-IN-1 is a kinase inhibitor (Flavopiridol analogue) that effectively inhibits HsGSK3β, HsCDK9/CyclinT, HsCDK5/p25 and HsCDK2/CyclinA with IC50 values of 59 nM, 64 nM, 1.093 μM and 1.725 μM, respectively. CDK9/10/GSK3β-IN-1 exhibited comparable or higher anti-cancer cell activity than Flavopiridol and showed high anti-proliferative activity against up to seven cancer cell lines in vitro.

AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity.

AG-012986 HCl is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 HCl showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 HCl was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 HCl also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity.

QR-6401, a selective macrocyclic CDK2 inhibitor, is orally active with IC50 values of 0.37 nM for CDK2/E1, 10 nM for CDK9/T1, 22 nM for CDK1/A2, 34 nM for CDK6/D3, and 45 nM for CDK4/D1. It exhibits potent antitumor activity in the OVCAR3 ovarian cancer xenograft model, indicating its potential for use in cancer research [1].

PROTAC CDK9/CycT1 Degrader-1 (compounds 10), a potent CDK9 inhibitor and target protein ligand for PROTAC synthesis, exhibits substantial anti-proliferative activity in solid tumors [1], making it instrumental in the targeted degradation of CDK9/CycT1.