CDK

YK-2168 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 5.9 nM. By inhibiting the phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain, YK-2168 effectively induces apoptosis in tumor cells and suppresses the expression of CDK9-regulated genes, including MYC and Mcl1. This reagent is valuable for research applications in cancer biology, particularly in the study of leukemia and tumor growth inhibition in CDX mouse models.

KI-ARv-03 is a potent and selective ATP-competitive inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC₅₀ of 0.15 μM in the presence of 45 μM ATP, with over 130-fold selectivity for CDK9 relative to other CDKs. This compound effectively reduces androgen receptor (AR)-driven transcription and cellular proliferation in prostate cancer models. KI-ARv-03 is applicable in the study of various malignancies, including leukemia, pancreatic cancer, alveolar rhabdomyosarcoma, and castration-resistant prostate cancer. Additionally, it serves as a ligand for PROTAC synthesis, specifically for generating PROTAC KI-CDK9d-32.

CDK2/MDM2-IN-1 is a potent dual inhibitor targeting both CDK2 and MDM2, exhibiting an IC50 value of 2.60 nM for CDK2. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to simultaneously inhibit key regulatory proteins positions it as a promising candidate for studies focused on cell cycle regulation and apoptosis.

CDK9-IN-30 is a selective inhibitor of Cyclin-dependent kinase 9 (CDK9), primarily targeting its role in transcription regulation. This compound exhibits potent antiviral activity by disrupting HIV-1 replication, making it a valuable tool for studying HIV-1 pathogenesis and exploring therapeutic strategies. Its inhibition of CDK9 can also provide insights into broader cellular processes related to transcriptional regulation and oncogenesis.

HZ1 is a selective inhibitor of cyclin-dependent kinase-like 3 (CDKL3) that operates via targeted inhibition of this kinase. It demonstrates significant tumor-suppressive activity and has potential to circumvent resistance to CDK4/6 inhibitors. This compound is applicable in cancer research, particularly in studies focused on cell cycle regulation and therapeutic resistance mechanisms.

Ribociclib succinate is an orally active inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), functioning through ATP-competitive mechanisms. It demonstrates potent activity with IC50 values of 10 nM and 39 nM against CDK4 and CDK6, respectively, while exhibiting over 1,000-fold selectivity against the cyclin B/CDK1 complex. This selectivity makes it a valuable tool in cancer research, particularly in studies targeting cell cycle regulation and therapeutic strategies for hormone receptor-positive breast cancer.

Ribociclib succinate hydrate is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), functioning through competitive inhibition of ATP binding. With IC50 values of 10 nM and 39 nM against CDK4 and CDK6, respectively, it demonstrates significant selectivity over the cyclin B/CDK1 complex. This compound is utilized in cancer research, particularly in studies focusing on cell cycle regulation, tumor proliferation, and the therapeutic potential in various malignancies. Its ability to cross the blood-brain barrier allows for exploration in central nervous system-related cancers.