cdk9 in 9

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

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

PROTAC CDK9 degrader-9 (compound 29) is a highly efficient, selective degrader of CDK9 based on PROTAC technology. It is utilized in cancer research.

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-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 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.

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/HDAC1/HDAC3-IN-1 is a dual inhibitor targeting CDK9 and HDAC enzymes. It potently suppresses the activity of CDK9, HDAC1, and HDAC3, with IC50 values of 0.17 μM, 1.73 μM, and 1.11 μM, respectively. The compound inhibits cancer cell growth by inducing apoptosis and causing cell cycle arrest at the G2/M phase. In a mouse model using TNBC MDA-MB-231 xenografts, it effectively hinders tumor progression. This compound exhibits broad-spectrum anticancer effects, notably against breast cancer, cervical cancer, and liver cancer.

CDK9/EZH2-IN-1 is a dual-target inhibitor of CDK9 and EZH2 with IC50 values of 83.9 nM and 108.6 nM, respectively. It induces apoptosis and causes DNA double-strand breaks (DSB). Additionally, CDK9/EZH2-IN-1 inhibits the proliferation of MKN45, MDA-MB-453, and SW620 cancer cells, with respective IC50 values of 136.3 nM, 171.3 nM, and 315.7 nM.

CDK9degrader-1 is a selective CDK9 degrader (DC50: 0.4073 µM). It recruits ATG101 to initiate the autophagy-lysosome pathway and forms autophagosomes by recruiting LC3, which then fuse with lysosomes to degrade CDK9 and its partner protein, Cyclin T1 (DC50: 1.215 µM). CDK9degrader-1 induces caspase 3-mediated apoptosis and exhibits antitumor activity in a mouse HCT116 xenograft model.

CDK9 Antagonist-1 (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|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

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.

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

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.

CDK9/CycT1-IN-93 is a highly specific, ATP-competitive inhibitor of CDK9/CycT1 with antiviral activity.

PROTAC FLT3/CDK9 degrader-1, a potent dual degrader of FLT3 and CDK9, effectively induces apoptosis and targets protein degradation of FLT3 and CDK9. This compound holds research potential for FLT3-ITD mutated AML [1].

PROTAC CDK9 degrader-5 is a selective PROTAC that mediates degradation of CDK9 via the proteasome pathway, efficiently degrading CDK9 42 and CDK9 55 isoforms with DC50 values of 0.10 μM and 0.14 μM, respectively [1].

PROTAC CDK9 degrader-6 is a specific PROTAC targeting CDK9 for degradation via the proteasome pathway, effectively degrading CDK9 with DC50 values of 0.10 μM and 0.14 μM for the CDK9 42 and CDK9 55 isoforms, respectively [1].

PROTAC CDK9 degrader-7 is a proteolysis-targeting chimera (PROTAC) engineered to selectively target and mediate the degradation of Cyclin-Dependent Kinase 9 (CDK9) via the proteasome pathway [1].

PROTAC CDK9 Degrader-8 (Compound 21) is a potent degrader of CDK9 with an IC50 of 0.01 μM, utilized in cancer research [1].

PROTAC CDK9/CycT1 Degrader-2 inhibits CDK9 with an IC50 of 45 nM [1].