cdk9 in 1

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

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.

EGFR HER2 CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR, HER2, and CDK9, with IC50 values of 90.17 nM, 131.39 nM, and 67.04 nM, respectively, and exhibits 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.

CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC MDA-MB-231 cells with an IC50 of 0.044 μM and inducing apoptosis. This compound diminishes CDK9 transcriptional activity and downregulates phosphorylation of RNA Pol II CTD ser2. In vivo, CDK9-Cyclin T1 PPI-IN-1 effectively impedes tumor growth in a TNBC 4T1 mouse model [1].

Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and effectively blocks CDK9, the transcriptional regulator of MCL-1.

LSN2839567 (Abemaciclib metabolite M2) is the active metabolite of Abemaciclib, a potent CDK4 and CDK6 inhibitor (IC50s: 1-3 nM) with anticancer activity.LSN2839567 inhibits CDK9.LSN2839567 inhibits cell growth and cell cycle progression in a concentration-dependent manner. cell growth and cell cycle progression in a concentration-dependent manner and can be used to study breast and lung cancer.

CDK8 19-IN-1 is a selective, orally bioavailable dual inhibitor of CDK8 and CDK19, with IC50 values of 0.46 nM for CDK8, 0.99 nM for CDK19, and 270 nM for [CDK9].

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

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].

CDK2 9-IN-1 (compound 20a) is an orally active dual inhibitor of CDK2 and CDK9, with IC50 values of 0.004 μM and 0.009 μM for CDK2 and CDK9, respectively. It induces apoptosis by regulating G2 M cell cycle arrest and exhibits antitumor activity.

LC3B ligand 1 is the target protein ligand for PROTAC, and it can be utilized in the synthesis of PROTACCDK9 autophagic degrader 1.

CDK4 9-IN-1 (Compound 29) is a selective dual inhibitor of CDK4 and CDK9, exhibiting IC50 values of 23 nM and 12 nM, respectively. It holds potential for use in cancer research.

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.

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).

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.

BUR1 is a selective BMP upregulator that acts by increasing the expression of Inhibitor of DNA binding 1 and inducing BMP2 and PTGS2 expression.

CDK7 9 tide is a peptide substrate for CDK7 or CDK9[1].

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

CDK6 9-IN-1 (compound 66) is a potent, orally administered dual inhibitor of CDK6 and CDK9, with IC50 values of 40.5 nM and 39.5 nM, respectively.

CDK7 9-IN-1 is a specific inhibitor of cyclin-dependent kinases 7 9 (CDK7 9), targeting CDK7 with IC50 values of 0.0656 μM without pre-incubation and 0.00574 μM after 3 hours pre-incubation, and displaying inhibitory activity against CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation, making it valuable for cancer research.