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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.
AG-12275 is a selective cyclin-dependent kinase (CDK) inhibitor that targets CDK2 and CDK5. It exhibits potent inhibition of cancer cell proliferation by disrupting the cell cycle progression. This compound is valuable for investigating the roles of CDKs in cancer biology and the development of novel therapeutic strategies targeting these pathways.
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CDK9-IN-46 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), which plays a crucial role in transcriptional regulation. This compound demonstrates significant biological activity in reducing the phosphorylation of RNA polymerase II, thereby inhibiting gene transcription associated with cancer cell proliferation. CDK9-IN-46 is utilized in cancer research to explore therapeutic strategies targeting CDK9-dependent pathways.
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CDK4/6-IN-16 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), exhibiting a potent activity with an IC50 of 0.013 μM for CDK4. This compound has significant implications for the study of CDK4-mediated pathologies, particularly in cancer research. Its targeted inhibition of CDK4/6 may aid in the exploration of cell cycle regulation and therapeutic strategies for cancer treatment.
(S)-Cdc7-IN-18 is a selective inhibitor of CDC7, a critical kinase involved in cell cycle regulation. By inhibiting CDC7, (S)-Cdc7-IN-18 effectively reduces the overactivation of MCM2, a key marker associated with tumor cell proliferation. This compound shows promise for research applications focused on cancer biology and therapeutic strategies aimed at countering tumorigenesis.
YY173 is a selective dual inhibitor of CDK4 and CDK6, demonstrating IC50 values of 7.7 nM and 88 nM, respectively. This compound effectively inhibits the proliferation of Jurkat cells with an IC50 of 1.46 μM. YY173 serves as a valuable tool for research in cancer biology and is suitable for the synthesis of PROTAC CDK4/6 degrader 1, facilitating studies on targeted protein degradation.
CDK7-IN-12 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), which is integral to transcriptional regulation and cell cycle control. This compound demonstrates significant capacity to impede the proliferation of malignant tumors in both in vitro and in vivo studies. CDK7-IN-12 is suitable for research applications focused on cancer biology and therapeutic development.
CDK2-IN-36 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), a crucial regulator of the cell cycle. This compound exhibits significant anticancer activity by disrupting CDK2-mediated phosphorylation events, thereby promoting apoptosis and inhibiting tumor cell proliferation. CDK2-IN-36 is valuable for research focused on cancer biology, cell cycle regulation, and the development of targeted cancer therapies.
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CDK12/13-IN-2 is a covalent inhibitor targeting cyclin-dependent kinases 12 and 13, with IC50 values of 15.5 nM and 12.2 nM for CDK12 and CDK13, respectively. This compound effectively inhibits the proliferation of breast cancer cells and is particularly relevant for research into triple-negative breast cancer. Its selective action provides a valuable tool for studying the effects of CDK12/13 inhibition in cancer biology.
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CDK2-IN-46 is a highly selective cyclin-dependent kinase 2 (CDK2) inhibitor with an IC50 value of 0.3 nM. It demonstrates a significant selectivity of over 200-fold compared to other kinases, including CDK1, CDK4, CDK6, CDK7, and CDK9. This compound is valuable for studying cell cycle regulation and has shown improved pharmacokinetic profiles in both rat and cynomolgus monkey models, making it suitable for preclinical research in cancer biology and therapeutic development.
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CDK2-IN-18 is a potent inhibitor of cyclin-dependent kinases CDK2/E and CDK4/D1, exhibiting IC50 values of 8 nM and 46 nM, respectively. This compound effectively inhibits tumor cell proliferation, making it valuable for cancer research applications, particularly in studying cell cycle regulation and exploring therapeutic strategies targeting CDK pathways.
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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.
