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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.
Cdc7-IN-19 is a highly potent inhibitor of CDC7, exhibiting an IC50 of 1.49 nM. This compound disrupts the kinase activity of CDC7, playing a critical role in the regulation of DNA replication and cell cycle progression. It is valuable for studying the molecular mechanisms of cancer, particularly in the development of targeted therapies that influence cell proliferation.
CDK7-IN-15 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), a key regulator of transcription and cell cycle progression. This pyrimidinyl derivative exhibits potent inhibitory activity, making it a valuable tool for investigating transcriptional dysregulation in various cancer types. CDK7-IN-15 is particularly relevant for cancer research focused on therapeutic strategies targeting aberrant transcriptional control.
Synonyms: CDK2-IN-26
RLY-2139 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2). By selectively targeting CDK2, it disrupts cell cycle progression, making it a valuable tool for studying cell division and proliferation. RLY-2139 has potential applications in cancer research, particularly in exploring therapeutic strategies for CDK2-related malignancies.
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rel-(2S,3R)-Voruciclib hydrochloride is the rel-(2S,3R)-enantiomer of Voruciclib, a potent inhibitor of cyclin-dependent kinases (CDKs). This compound exhibits significant biological activity in regulating cell cycle progression and has potential applications in cancer research, particularly in therapeutic strategies targeting CDK-mediated pathways. Its oral bioavailability makes it a valuable tool for in vivo studies of cell proliferation and tumor growth.
Cyclin A/B RxL-IN-2 is a macrocyclic peptide that acts as a selective inhibitor of Cyclin A and Cyclin B. It exhibits high potency with an IC50 of 0.05 μM for Cyclin A and less than 0.02 μM for Cyclin B, alongside Kd values of 2.7 nM and 1.0 nM, respectively. This compound competes for binding at the hydrophobic patch of Cyclin A/B, disrupting interactions with the substrate RxL motif, leading to replication stress and DNA damage in E2F-high cells, as well as inducing mitotic catastrophe and apoptosis. Cyclin A/B RxL-IN-2 demonstrates efficacy in inhibiting tumor growth in NCI-H69 and NCI-H446 small cell lung cancer xenograft models, making it a valuable tool for research in small-cell lung cancer.
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PRT3645 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). It demonstrates potent inhibition with IC50 values less than 20 nM, making it a valuable tool for studying cell cycle regulation and cancer biology. PRT3645 is primarily utilized in research applications targeting tumor cell proliferation and therapeutic strategies for cancers associated with dysregulated CDK4/6 activity.
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Cdc7-IN-8 is a potent inhibitor of Cdc7, a serine/threonine kinase essential for the activation of the MCM protein, which plays a critical role in the initiation of DNA replication. By blocking Cdc7 activity, Cdc7-IN-8 exhibits significant potential in cancer research by disrupting DNA replication processes. This compound serves as a valuable tool for investigating the mechanisms of oncogenesis and evaluating therapeutic strategies targeting cell proliferation.
GW780056X is a selective inhibitor of Cyclin-Dependent Kinase 12 (CDK12). It is known to reduce nuclear foci count in DM1 cells, demonstrating its potential in therapeutic strategies for myotonic dystrophy type 1. This compound serves as a valuable tool for investigating the molecular mechanisms underlying this genetic disorder and evaluating potential treatment options.
CDK8-IN-18 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8) with an IC50 of 43 μM. This compound is instrumental in studying the regulatory roles of CDK8 in transcription and its implications in oncogenesis. CDK8-IN-18 is widely used in cancer research to explore the therapeutic potential of targeting CDK8 in malignancies.
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CDK7/9-IN-1 is a potent inhibitor of cyclin-dependent kinases 7 and 9, demonstrating a selective inhibition profile that favors CDK7. This compound exhibits IC50 values of 0.0656 μM and 0.00574 μM for CDK7 without and with 3 hours of pre-incubation, respectively, while inhibiting CDK9 with an IC50 of 2.14 μM after pre-incubation. CDK7/9-IN-1 is valuable for research applications related to cancer, particularly in studies targeting the regulation of transcription and cell cycle progression mediated by these kinases.
CDK12-IN-7 is a potent inhibitor of cyclin-dependent kinases CDK12 and CDK2, exhibiting IC50 values of 42 nM and 196 nM, respectively. This compound demonstrates significant anti-cell proliferation activity, making it valuable for cancer research applications. Its selective inhibition of CDK12 may provide insights into tumorigenesis and potential therapeutic strategies in oncology.
BAY-958 is a potent inhibitor of PTEFb/CDK9, demonstrating high selectivity within the cyclin-dependent kinase family. This compound exhibits significant antiproliferative effects against various cancer cell lines, including HeLa and MOLM-13. Additionally, BAY-958 shows favorable metabolic stability and effectively reduces tumor growth in mouse xenograft models while maintaining a low toxicity profile, making it a valuable tool for cancer research.
CDK7-IN-26 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7) with an IC50 of 7.4 nM. This compound demonstrates significant efficacy in inhibiting the proliferation of triple-negative breast cancer (TNBC) cell line-derived xenograft tumors in vivo. In vitro studies show that CDK7-IN-26 effectively targets MDA-MB-453 cells, exhibiting an IC50 of 0.15 μM, making it a valuable tool for cancer research focusing on CDK7 inhibition.
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CDK12-IN-4 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), exhibiting a potent inhibitory effect with an IC50 of 0.641 μM at elevated ATP levels (2 mM). This compound demonstrates no significant activity against CDK2/Cyclin E or CDK9/Cyclin T1, with IC50 values exceeding 20 μM under the same conditions. CDK12-IN-4 is valuable for research into transcription regulation and therapeutic targeting in cancer biology, particularly in studies involving DNA damage and repair pathways.
Cdc7-IN-21 is a highly potent and selective inhibitor of Cdc7 with an IC50 of 0.07 nM. This compound is primarily utilized in cancer research, facilitating investigations into cell cycle regulation and potential therapeutic strategies targeting Cdc7-dependent pathways. Its specificity makes it a valuable tool for elucidating the role of Cdc7 in tumorigenesis and exploring new avenues for cancer treatment.
Ulecaciclib is an orally active inhibitor of cyclin-dependent kinases (CDKs), specifically targeting CDK2, CDK4, CDK6, and CDK7 with Ki values of 0.62 μM, 0.2 nM, 3 nM, and 0.63 μM, respectively. This compound exhibits excellent pharmacokinetic properties and is capable of crossing the blood-brain barrier. Ulecaciclib is valuable for research applications in cancer biology, particularly in the study of cell cycle regulation and CDK-related pathways in various malignancies.
CDK12-IN-9 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12) with an IC50 of 2.2 nM. This compound effectively inhibits phosphorylated serine 2 (pSER2), a key downstream marker associated with CDK12/13 activity. CDK12-IN-9 is suitable for cancer research, offering potential insights into therapeutic strategies targeting transcriptional regulation and DNA repair mechanisms in malignant cells.
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CDK2-IN-28 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), designed to modulate cell cycle progression. This compound demonstrates significant anti-proliferative activity against MKN1 cells, with an EC50 of 0.31 μM. CDK2-IN-28 is valuable for research into mechanisms of cell cycle regulation and potential therapeutic applications in cancer.
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CDK2-IN-51 is a pyrazolopyridine derivative that selectively inhibits cyclin-dependent kinase 2 (CDK2) with an IC50 value of 23.47 nM. This compound demonstrates significant biological activity by downregulating the expression of critical DNA replication factors, including Polα, MCM7, ORC2, and ORC4, leading to pre-G1 cell cycle arrest. CDK2-IN-51 is primarily utilized in the research of colorectal cancer, providing valuable insights into cell cycle regulation and potential therapeutic strategies.
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SR-5037 is an orally active inhibitor of CDK12 and CDK13, with an IC50 of 31 nM, and functions as a molecular glue degrader for CycK, demonstrating a DC50 of 30 nM and Dmax exceeding 98%. By inhibiting the enzymatic activity of the CDK12/CycK and CDK13/CycK complexes, SR-5037 facilitates the recruitment of DDB1, leading to proteasome-mediated degradation of CycK. This compound has shown efficacy in degrading active CycK in mouse models of triple-negative breast cancer and is a valuable tool for investigating treatment options in such malignancies.
CDK7-IN-17 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), a key regulator of transcription and cell cycle progression. This pyrimidinyl derivative demonstrates potent inhibitory activity against CDK7, making it a valuable tool in cancer research, particularly in studies related to transcriptional dysregulation in various malignancies. Its application in elucidating CDK7's role in tumorigenesis may provide insights into novel therapeutic strategies for cancer treatment.
CDK7-IN-31 is a highly potent and orally bioavailable inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating a Kd value of 0.18 nM. This compound exhibits significant anticancer activity, making it a valuable tool for cancer research and therapeutic development. Its selective inhibition of CDK7 facilitates investigations into the role of this kinase in cell cycle regulation and transcriptional control.
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CDK8-IN-14 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), displaying an IC50 value of 39.2 nM. This compound demonstrates significant anti-proliferative effects on acute myeloid leukemia (AML) cells, with reported GC50 values of 0.02 ± 0.01 μM for Molm-13 and 0.03 ± 0.01 μM for MV4-11. Its potency makes it a valuable tool for research into CDK8-mediated signaling pathways and potential therapeutic strategies in AML.
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CDK4/6-IN-8 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), displaying IC50 values of 5.01 nM and 3.97 nM for each target, respectively. This compound effectively modulates cell cycle progression, making it a valuable tool for studies related to cancer biology and therapies targeting cell proliferation. Its precise inhibition of CDK4 and CDK6 positions it for use in research on tumor cell growth and the mechanistic exploration of cell cycle dysregulation in various malignancies.
CDK12-IN-8 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), which primarily targets the phosphorylation of the C-terminal domain (CTD) serine 2 of RNA polymerase II. By disrupting CDK12-mediated transcription elongation and DNA damage repair mechanisms, CDK12-IN-8 has significant implications for cancer research, particularly in malignancies characterized by elevated CDK12 expression, such as small cell lung cancer and triple-negative breast cancer. It serves as a valuable tool for exploring the role of CDK12 in oncogenic processes.
