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CDK inhibitors block cyclin-dependent kinases (CDKs), the serine/threonine kinases that drive the cell cycle. Each CDK becomes active only when bound to a cyclin partner, and successive cyclin-CDK complexes order DNA replication and mitosis. CDK4 and CDK6 pair with D-type cyclins to control progression through G1, while CDK1 governs entry into mitosis. Palbociclib and abemaciclib are selective CDK4/6 inhibitors used to study G1 arrest and retinoblastoma protein phosphorylation. Dinaciclib and seliciclib act on several family members, including CDK2, CDK5 and CDK9, which also links them to transcription research. Ro 3306 inhibits CDK1 and is used to hold cells reversibly at the G2/M boundary for synchronization experiments.
ZK 304709 is a multi-target cyclin-dependent kinase (CDK) inhibitor that plays a critical role in cell cycle regulation. It effectively inhibits various CDKs, thereby preventing proliferation in cancer cells. This compound is valuable for studying mechanisms of cell cycle control and can aid in the development of novel therapeutic strategies against cancer.
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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.
CDK7 ligand 2 is a selective inhibitor targeting CDK7, a crucial cyclin-dependent kinase involved in transcription regulation. This compound exhibits significant potential in drug discovery and development, particularly in the synthesis of PROTACs (Proteolysis Targeting Chimeras). Its application in research may facilitate novel therapeutic approaches for diseases associated with abnormal transcriptional control.
CDK9 ligand 4 functions as a potent ligand for cyclin-dependent kinase 9 (CDK9). This compound is instrumental in the design and development of PROTAC-based degraders, facilitating targeted degradation of CDK9 proteins, which plays a crucial role in transcriptional regulation and HIV-1 infection research. CDK9 ligand 4 contributes significantly to studies aimed at therapeutic strategies against viral infections and dysregulated transcriptional processes.
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CDK4 Degrader 1 (ML 1–71) is a molecular glue degrader that specifically targets cyclin-dependent kinase 4 (CDK4). This compound promotes the selective degradation of CDK4, leading to reduced cell proliferation and induction of cell cycle arrest in various cancer models. It serves as a valuable tool for investigating CDK4's role in tumorigenesis and for the development of targeted therapies in cancer research.
PROTAC CDK9 degrader-4 is a potent CDK9 degradation agent that facilitates the targeted degradation of cyclin-dependent kinase 9. This compound effectively modulates transcriptional regulation by harnessing the power of PROTAC technology, leading to significant biological activity in various cellular contexts. It holds potential applications in cancer research and the study of transcriptional control mechanisms.
Synonyms: (S)-NG 95
(S)-Purvalanol B is the S enantiomer of Purvalanol B, a selective inhibitor of cyclin-dependent kinases (CDKs). This compound effectively disrupts the activity of CDKs, which play a critical role in cell cycle regulation and cellular proliferation. Due to its unique targeting mechanism, (S)-Purvalanol B is valuable in cancer research, particularly in studies related to cell cycle dysregulation and therapeutic strategies for tumor proliferation control.
Iso-Olomoucine is an inactive stereoisomer of the CDK5 inhibitor olomoucine, exhibiting an IC50 value greater than 1 mM. It serves as a valuable control in experiments assessing CDK5 activity and modulation. This compound is primarily used in research applications focused on neurological disorders and cell cycle regulation, providing insights into the mechanisms of CDK5 inhibition.
CDK8-IN-2 is a potent inhibitor of cyclin-dependent kinase 8 (CDK8) with an IC50 value of 0.010 μM, and it also demonstrates activity against CDK19 with an IC50 of 0.026 μM. This compound effectively inhibits phospho-STAT1, serving as a pharmacodynamic biomarker for CDK8 activity, while also reducing WNT pathway activity. CDK8-IN-2 is suitable for research focused on colorectal carcinoma and offers insights into CDK8's role in tumorigenesis and cellular signaling pathways.
CDK7-IN-33 is an inhibitor of CDK7 kinase, characterized by its pyrimidine structure. This compound demonstrates potent inhibitory activity, making it valuable in research applications related to cancer, inflammation, cardiovascular diseases, infectious diseases, immune disorders, and metabolic conditions. Its selective modulation of CDK7 activity highlights its potential for therapeutic exploration in various pathological contexts.
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CTX-439 is a potent, orally active ATP-competitive inhibitor targeting CDK12 and CDK13, with an IC50 of 3.1 nM for CDK12 and 9.2 nM for CDK13. This small-molecule compound is effective in inducing DNA damage and apoptosis in tumor cells. CTX-439 is particularly relevant for research focused on breast and ovarian cancer therapies.
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CDK9 Ligand 5 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), a critical regulator of transcriptional control. This compound serves as a valuable ligand for the design and development of PROTACs (Proteolysis Targeting Chimeras) aimed at degrading CDK9, exemplified by the PROTAC CDK9 degrader-9. CDK9 Ligand 5 is particularly relevant in cancer research, where CDK9 activity plays a pivotal role in cell proliferation and survival.
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PROTAC CDK2-pRb degrader-1 is an orally active PROTAC that targets cyclin-dependent kinase 2 (CDK2) for degradation. This compound effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine 807/811 by promoting the ubiquitination and proteasomal degradation of CDK2. Demonstrating significant biological activity with EC50 values of 12 nM and 125 nM in human cells, PROTAC CDK2-pRb degrader-1 is particularly useful in research focused on CCNE1-amplified cancers, including ovarian, gastric, and breast cancers, as it inhibits tumor growth and induces tumor stasis in xenograft models.
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CDK2-IN-56 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2). This compound, classified as a pyrazoloquinazoline-3-carboxamide, demonstrates significant inhibitory activity against CDK2 while also affecting cyclin A. CDK2-IN-56 is primarily utilized in cancer research, providing valuable insights into cell cycle regulation and potential therapeutic strategies targeting CDK2-related pathways.
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