cdk 9

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

CDK9-IN-8 is a highly potent and selective CDK9 inhibitor (IC50: 12 nM).

CDK9-IN-2 is a specific CDK9 inhibitor with an IC50 of 5 nM in the A2058 skin cell line (72 hours) and 7 nM in the H929 multiple myeloma cell line (72 hours).

CDK9-IN-15 is a potent small molecule CDK9 inhibitor, which can block the phosphorylation of positive transcription elongation factor b (P-TEFb) on the C-terminal region of RNA Poly-II by degradation and inhibition of CDK9, inhibit transcription, and rapidly reduce the level of intracellular mRNA, thereby causing apoptosis of tumor cells.

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

CDK9-IN-9 is a potent and selective CDK9 inhibitor (IC50: 1.8 nM) with anti-cancer activity. It inhibits CDK2 (IC50: 155 nM).

PROTAC CDK2/9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).

PROTAC CDK9 Degrader-1 is a selective PROTAC CDK9 degrader composed of a cereblon ligand and a CDK9 ligand.

CDK12-IN-E9 is a cell cycle protein kinase (CDK) inhibitor with anticancer and antitumor activity that can be used in the study of breast cancer.

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).

CDK9 inhibitor HH1 (8019-9719) is an inhibitor of the human CDK2-cyclin A2 complex with an IC50 value of 2 μM.

CDK9-IN-1 is a selective and potent CDK9 inhibitor with antiviral activity used in the study of PRRSV infections.

PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1].

CDK9-IN-12 is a highly selective CDK9 inhibitor, which is commonly used in leukemia research to regulate oncogene expression, inhibit oncogenic proliferation, and induce apoptosis by targeting CDK9-dependent transcription processes.

PROTAC CDK9 degrader 4 is a highly potent CDK9 degrader that targets transcriptional regulation and has potential anticancer activity for the study of acute myelogenous leukemia (AML).

PROTAC CDK9 ligand-1, a CDK9 ligand, is used in the synthesis of PROTACs.

CDK9-IN-34 (Compound 1b) is an inhibitor of CDK9 with an IC50 of 0.25 μM. It exhibits cytotoxicity against cancer cell lines HCT116, MCF7, and K652, with IC50 values of 1.43 μM, 3.01 μM, and 50.27 μM, respectively. Additionally, CDK9-IN-34 demonstrates antiviral activity against coronavirus 229E with an IC50 of 145.92 μM.

CDK9 autophagic degrader 1 (Compound 28) is an ATTEC degrader used to target and degrade CDK9, also impacting the levels of its associated Cyclin T1. At a concentration of 100 nM, it exhibits over 80% inhibition of CDK9.

CDK9-IN-36 (Compound T7) is a potent, selective, and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. It effectively suppresses the proliferation of Osimertinib-resistant NSCLC cells by downregulating Mcl-1, reducing colony formation, and inducing apoptosis. Additionally, CDK9-IN-36 exhibits antitumor activity in xenograft models.

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)

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

CDK9/PARP-IN-1 (compound 37) is an inhibitor of CDK9 and PARP. It demonstrates IC50 values of 118 nM for CDK9 and 107 nM for PARP1. This compound exhibits a broad-spectrum anti-proliferative effect across various cancer cell lines.

CDK9-IN-38 (compound 14) is a CDK9 inhibitor with IC50 values of 1.2 nM for wild-type CDK9 and 3.3 nM for the L156F mutant. It effectively inhibits tumor growth both in vitro and in vivo.

CDK9-IN-37 (Compound 24) is a CDK9 inhibitor with high selectivity, demonstrating an EC50 of 5.5 nM and minimal inhibition of other CDK subtypes. It shows significant antiproliferative activity against acute myeloid leukemia cells MOLM-13, with an IC50 of 0.034 μM. CDK9-IN-37 suppresses CDK9 signaling, reducing RNAP II CTD (Ser2) phosphorylation, downregulating the anti-apoptotic protein McI-1, inducing apoptosis, and causing cell cycle arrest at the G2/M phase. This compound is applicable in the research of acute myeloid leukemia (AML).