cdk9 in 11

CDK9-IN-11 is a potent CDK9 inhibitor and serves as the ligand for the PROTAC CDK9 Degrader-1 [1].

PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC CDK9 degrader with a DC50 of 1.09 nM. This compound exhibits cytotoxicity in small cell lung cancer (SCLC) cells, with IC50 values in the nanomolar range. It induces cell cycle arrest at the G0/G1 phase and inhibits cell invasion in DMS114 and DMS53 cells. In addition, PROTAC CDK9 degrader-11 shows antitumor activity in an NCI-H446 xenograft mouse model. (Pink: ligand for target protein CDK9 ligand 3; Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56)

CDK9-IN-7 is a highly selective and orally active CDK9/cyclin T inhibitor (IC50: 11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD: 148 nM; CDK6/cyclinD: 145 nM).

E3 Ligase Ligand 56 is a ligand for the E3 ligase Cereblon, and it can be utilized in the synthesis of [PROTACCDK9degrader-11].

CDK9ligand 3 is a ligand for CDK9 and can be utilized in the synthesis of PROTAC degraders, specifically PROTAC CDK9degrader-11.

HS-36 is a highly selective, orally bioavailable dual inhibitor of CDK4 and CDK9, with IC50 values of 18.9 nM and 4.2 nM, respectively. It exhibits potent nanomolar activity against various cancer cells, inducing G0/G1 phase arrest and promoting apoptosis. In MV-4-11 tumor mouse models, HS-36 effectively suppresses tumor growth and can be used for research in acute myeloid leukemia.

CDK9-IN-14 is a potent, high and low selective CDK9 inhibitor (IC50: 6.92 nM). CDK9-IN-14 is a strong inhibitor of MV-4-11 cells and in vivo tumour models with low toxicity and few side effects.

CDK9-IN-19 is a selective and potent CDK9 inhibitor (IC50: 2.0 nM). CDK9-IN-19 exhibits good anti-proliferative activity in cancer cells, moderate pharmacokinetic properties and low hERG inhibition. CDK9-IN-19 significantly inhibited tumor growth in the MV4-11 xenograft mouse model. CDK9-IN-19 can be used in studies of acute myeloid leukemia (AML).

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.