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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.
CDK-IN-15 is a potent inhibitor of Cyclin A, exhibiting an IC50 value of 0.14 μM. This compound is useful for studying cell cycle regulation and the inhibition of cyclin-dependent kinases in cancer research. Its biological activity makes it a valuable tool in investigating the role of Cyclin A in various cellular processes and the development of novel therapeutic strategies.
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Tacaciclib is a selective cyclin-dependent kinase (CDK) inhibitor that exerts antineoplastic effects by disrupting cell cycle progression. It primarily targets CDK2 and CDK9, leading to the inhibition of cancer cell proliferation. This compound is useful in cancer research for exploring therapeutic pathways and mechanisms of resistance in tumor models.
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CDK8-IN-7 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), exhibiting a Kd of 3.5 nM. This compound demonstrates notable cytotoxicity across various cancer cell lines, including MOLM-13, OCI-AML3, MV4-11, NRK, and H9c2, with IC50 values ranging from 4.8 to 25 µM. CDK8-IN-7 is a valuable tool for investigating the role of CDK8 in acute myeloid leukemia (AML) and other related malignancies.
CDK2/4-IN-2 is a potent dual inhibitor of cyclin-dependent kinases 2 and 4, exhibiting IC50 values below 100 nM. This compound is instrumental in cancer research, providing insights into cell cycle regulation and the therapeutic potential of targeting CDK pathways. Its efficacy in inhibiting CDK2 and CDK4 makes it a valuable reagent for investigating tumor cell proliferation and developing anti-cancer strategies.
rel-(2S,3R)-Voruciclib is a selective cyclin-dependent kinase (CDK) inhibitor, specifically the (2S,3R)-enantiomer of Voruciclib. This compound exhibits potent inhibition of CDK activity, making it valuable for the study of cell cycle regulation and cancer therapeutics. Its oral bioavailability allows for convenient administration in research applications focused on tumor growth inhibition and cell proliferation modulation.
CDK7-IN-25 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7) with an IC50 of less than 1 nM. This compound plays a critical role in regulating transcription and cell cycle progression, making it a valuable tool in cancer research. CDK7-IN-25 can be utilized to investigate the effects of CDK7 inhibition on tumor cell proliferation and survival, as well as to explore its potential therapeutic applications in oncology.
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CDK2-IN-7 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), providing valuable insights into cancer biology. With an IC50 of less than 50 nM, it effectively disrupts CDK2 activity, facilitating studies on cell cycle regulation and tumor progression. This compound is useful for researchers investigating CDK-targeted therapies and cell proliferation in various cancer models.
CDK4/6-IN-21 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), exhibiting IC50 values of 3.88 nM and 3.31 nM for CDK4 and CDK6, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research, particularly in studies targeting cell cycle regulation and proliferation in various malignancies. Its potent inhibition of CDK4 and CDK6 positions it as a promising candidate for therapeutic development in oncology.
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CDK4/6-IN-5 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6), exhibiting binding affinities (Kis) of 0.2 nM for the CDK4/Cyclin D1 complex and 4.4 nM for the CDK6/Cyclin D3 complex. This compound demonstrates significant biological activity in interrupting cell cycle progression, making it a valuable tool for cancer research, especially in studies focused on tumor proliferation and therapeutic resistance mechanisms. Its potency and selectivity make CDK4/6-IN-5 an important reagent for investigating the roles of CDK4 and CDK6 in various cancer types.
CDK8-IN-5 is a potent inhibitor of cyclin-dependent kinase 8 (CDK8) with an IC50 of 72 nM. This compound exhibits significant anti-inflammatory activity, evidenced by a 43% enhancement in IL-10 levels. CDK8-IN-5 is applicable in research focusing on inflammatory bowel disease and related inflammatory conditions.
Anticancer agent 30, a 3-arylidene-2-oxindole derivative, functions primarily as a selective inhibitor of cyclin-dependent kinase 2 (CDK2). This compound exhibits potent anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to modulate CDK2 activity positions it as a promising candidate for investigations into cell cycle regulation and tumor progression.
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Cdc7-IN-18 is a selective inhibitor of the CDC7 kinase, demonstrating an IC50 of 1.29 nM against the Cdc7/DBF4 enzyme. This compound exhibits significant antiproliferative effects, with an IC50 value of 53.62 nM in COLO205 colorectal cancer cells. Its efficacy makes Cdc7-IN-18 a valuable tool for research in cell cycle regulation and cancer therapeutics.
AG-024104 is a potent cyclin-dependent kinase (CDK) inhibitor, demonstrating Ki values of 2.3 nM for CDK1/cyclin B, 1.8 nM for CDK2/cyclin A, and 0.67 nM for CDK4/cyclin D. By effectively inhibiting the kinase activity of these CDKs, AG-024104 is valuable in studying cell cycle regulation and cancer pathways. This inhibitor is also utilized as a negative control in peripheral leukocyte toxicity studies during preclinical development.
Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG) is a specific inhibitor of cyclin-dependent kinase 2 (CDK2). It has demonstrated the ability to induce apoptosis in U2OS osteosarcoma cells in a dose-dependent manner, making it a valuable tool for studying CDK2-mediated cell cycle regulation. This peptide is suitable for research applications aimed at understanding the role of CDK2 in cancer biology and potential therapeutic interventions.
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Cdc7-IN-12 is a potent inhibitor of the CDC7 kinase, exhibiting an IC50 of less than 1 nM. This compound demonstrates significant antiproliferative activity in COLO205 cells, with an IC50 range of 100-1000 nM. Cdc7-IN-12 is valuable for research in cancer biology, focusing on cell cycle regulation and potential therapeutic applications.
CDK-IN-19 is a potent cyclin-dependent kinase (CDK) inhibitor that selectively targets CDK enzymes involved in cell cycle regulation. This compound demonstrates significant antiproliferative activity and is valuable for cancer research applications, particularly in studying CDK-mediated pathways and the effects of cell cycle disruption in oncogenesis. Its role as a CDK inhibitor makes it a crucial tool for investigating therapeutic strategies aimed at cancer treatment.
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SNX2-1-108 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8). This compound plays a pivotal role in modulating transcriptional regulation and is essential for various cellular processes. Its inhibition of CDK8 activity has significant implications in cancer research, particularly in studying the regulatory pathways of gene expression and potential therapeutic interventions in CDK8-dependent malignancies.
EF-4-177 is an allosteric inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 87 nM. This compound effectively interferes with spermatogenesis, making it a valuable tool for studying male reproductive biology and the regulatory mechanisms of cell cycle progression. Its oral activity enhances its utility in pharmacological research and potential therapeutic applications.
SZ-015268 is a potent CDK7 inhibitor, exhibiting an IC50 of 23.56 nM. This compound demonstrates significant anti-tumor activity, effectively inhibiting the proliferation of various cancer cell lines, including HCC70 (IC50 33 nM), OVCAR-3 (IC50 80.56 nM), HCT116 (IC50 12.53 nM), and HCC1806 (IC50 61.55 nM). SZ-015268 serves as a valuable tool in cancer research, particularly in studies focused on cell cycle regulation and therapeutic strategies targeting CDK7.
PROTAC CDK9/CycT1 Degrader-2 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 45 nM. This compound promotes targeted protein degradation, thereby modulating transcriptional regulation and influencing cellular processes associated with gene expression. It is valuable for research applications focused on cancer biology and therapeutic development by addressing dysregulated CDK9 activity.
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CDK4/6-IN-22 is a potent dual inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). By inhibiting these kinases, CDK4/6-IN-22 effectively disrupts cell cycle progression, making it a valuable tool in cancer research. This compound is particularly relevant for studies exploring therapeutic strategies for tumors characterized by dysregulated CDK4/6 activity.
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Aloisine B is a potent cyclin-dependent kinase (CDK) inhibitor. It effectively inhibits cell proliferation by inducing cell cycle arrest in both the G1 and G2 phases through competition for the ATP-binding pocket. This compound serves as a valuable tool for research in cancer biology and cell cycle regulation.
Cyclin A/B RxL-IN-1 is an inhibitor that targets the interaction between Cyclin A/B and the hydrophobic patch (HP). With an IC50 of 0.12 μM, it effectively inhibits Cyclin A, demonstrating notable antitumor activity in cell line-derived xenograft (CDX) models. This compound is valuable for research on E2F-driven cancers, including small-cell lung cancer (SCLC), providing insights into therapeutic strategies.
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CDK2-IN-29 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 96 nM. Additionally, it shows activity against CDK4 with an IC50 of 360 nM. This compound is instrumental in the study of cell cycle regulation and has potential applications in cancer research, where CDK inhibition plays a critical role in controlling cell proliferation.
CDK7-IN-8 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating an IC50 of 54.29 nM. This compound effectively inhibits the proliferation of specific cancer cell lines and has shown promising activity in various in vivo tumor models. CDK7-IN-8 is utilized in research applications targeting cancer therapeutics and cell cycle regulation studies.
