cdk9 in 1

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

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

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

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

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

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

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].

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-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.

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-13 is a potent and selective CDK inhibitor (IC50<3 nM). CDK9-IN-13 has a very short half-life in rodents.

CDK9-IN-18, a potent inhibitor of CDK9, blocks its phosphorylation, exhibits good anticancer activity, induces apoptosis, and has low cellular activity.

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).

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.