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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.
CDKI-IN-1 is a potent cyclin-dependent kinase inhibitor (CDKI) designed for investigating the role of CDK modulation in central nervous system (CNS) degenerative diseases. It effectively inhibits CDK activity, thereby providing insight into cell cycle regulation and neuronal cell survival. This compound is valuable for exploring therapeutic strategies targeting CDK pathways in neuroscience research.
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Crozbaciclib fumarate is a potent inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), with IC50 values of 3 nM and 1 nM, respectively. This compound effectively regulates cell cycle progression by hindering the phosphorylation of retinoblastoma protein, thereby halting proliferation in various cancer cell lines. Crozbaciclib fumarate is utilized in oncology research, particularly in studies investigating the therapeutic potential of targeting CDK4/6 in tumor growth and resistance mechanisms.
Synonyms: BAY-958 hydrochloride
BAY-1112054 hydrochloride is a potent inhibitor of PTEFb/CDK9, demonstrating high selectivity within the cyclin-dependent kinase family. This compound exhibits significant antiproliferative activity against various cancer cell lines, including HeLa and MOLM-13. BAY-1112054 hydrochloride is characterized by good metabolic stability and effectively suppresses tumor growth in mouse xenograft models while maintaining a favorable toxicity profile. Its mechanism and efficacy make it a valuable tool for cancer research applications.
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Synonyms: PROTAC CDK4/6 degrader 34
CST651 is a selective proteolysis-targeting chimera (PROTAC) degrader specifically designed to target cyclin-dependent kinases CDK4 and CDK6. This compound effectively degrades CDK4 and CDK6 in MM.1S cells, exhibiting DC50 values of 20 nM and 5.1 nM, respectively. CST651 demonstrates the ability to inhibit cancer cell proliferation and migration, making it a valuable tool for research into various cancers, including acute lymphoblastic leukemia.
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SLM6 is a potent CDK9 inhibitor, specifically targeting the CDK9/cyclin K and CDK9/cyclin T1 complexes with IC50 values of 280 nM and 133 nM, respectively. In addition, SLM6 also effectively inhibits CDK1/cyclin B and CDK2/cyclin A, demonstrating IC50 values below 300 nM. This compound has been shown to induce apoptosis in multiple myeloma cells, making it a valuable tool for research in cancer biology and therapeutic development for hematological malignancies.
Xylocydine is a potent inhibitor of cyclin-dependent kinases CDK1 and CDK2, demonstrating IC50 values of 1.4 nM and 61 nM, respectively. This compound effectively disrupts CDK activity, contributing to the regulation of apoptotic processes. Additionally, Xylocydine downregulates the levels of phosphorylated nucleolin and retinoblastoma protein, making it a valuable tool for investigations into cell cycle regulation and cancer research.
CDK7-IN-18 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7). This pyrimidinyl derivative exhibits significant potential in the investigation of various cancers, particularly those associated with transcriptional dysregulation. CDK7-IN-18 serves as a valuable tool for research applications focused on understanding tumorigenesis and exploring therapeutic strategies targeting CDK7-mediated pathways.
CDK2-IN-8 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 value of 1.74 µM. This compound demonstrates significant antiproliferative activity, making it a valuable tool for studying cancer biology. CDK2-IN-8 is particularly relevant for research applications focused on melanoma and related malignancies, where CDK2 activity plays a crucial role in cell cycle regulation and tumor progression.
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CDK5-IN-2 is a highly selective cyclin-dependent kinase 5 (CDK5) inhibitor, exhibiting IC50 values of 0.2 nM against CDK5/p25 and 23 nM against CDK2/CycA. It serves as a valuable tool in research focused on neurodegenerative diseases, as CDK5 plays a critical role in neuronal function and development. This compound enables the exploration of CDK5's involvement in various cellular processes and its potential as a therapeutic target.
Cdc7-IN-14 is a highly potent inhibitor of CDC7, exhibiting an IC50 of less than 1 nM. This compound demonstrates significant efficacy in disrupting the regulation of cell cycle progression, making it a valuable tool for cancer research. Its ability to inhibit CDC7 offers insights into the underlying mechanisms of tumor cell proliferation and underscores its potential in therapeutic applications.
CDK2 Degrader 8 is a novel chemical probe designed to target and degrade cyclin-dependent kinase 2 (CDK2). By specifically modulating CDK2 levels, it demonstrates significant anti-tumor activity, making it a valuable tool for investigating solid tumors such as breast cancer and ovarian serous cystadenocarcinoma, as well as liquid tumors like diffuse large B-cell lymphoma and acute myelogenous leukemia. CDK2 Degrader 8 facilitates research into the pathological roles of CDK2 dysregulation in cancer.
Cdc7-IN-13 is a potent inhibitor of CDC7 with an IC50 of less than 1 nM, demonstrating significant enzymatic activity inhibition. This compound is primarily utilized in cancer research to investigate the role of CDC7 in cell cycle regulation and its implications in tumorigenesis. Cdc7-IN-13 offers a valuable tool for exploring therapeutic strategies targeting cell division in various malignant cell lines.
TrkA Inhibitor is a selective CDK2 inhibitor, demonstrating an IC50 of 0.69 μM against CDK1. This compound is particularly valuable in research focused on chemotherapy-induced alopecia, allowing for the investigation of mechanisms involved in hair follicle cycling and potential therapeutic interventions. Its specificity for CDK2 makes it a useful tool in examining cell cycle regulation and associated pathways in various biological contexts.
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CDK9-IN-19 is a selective inhibitor of Cyclin-Dependent Kinase 9 (CDK9), exhibiting a potent IC50 value of 2.0 nM. This compound demonstrates significant antiproliferative activity in cellular assays and effectively suppresses tumor growth in MV4-11 xenograft models. With moderate pharmacokinetic properties and minimal hERG inhibition, CDK9-IN-19 is valuable for research on acute myeloid leukemia (AML) and related oncogenic pathways.
CDK9-IN-22 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9) with an IC50 of 10.4 nM for CDK9, demonstrating significant efficacy in disrupting cellular pathways. This compound is known to induce apoptosis and promote cell cycle arrest at the G2/M phase. Additionally, CDK9-IN-22 decreases the levels of phosphorylated RNA polymerase II (S2) and CDK9 protein, exhibiting notable antiproliferative and anti-tumor properties. It is a valuable tool for research in cancer biology and therapeutic applications targeting CDK9-related pathways.
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P18IN005 hydrochloride is a selective inhibitor of cyclin-dependent kinase (CDK), primarily targeting p18. This compound effectively regulates hematopoietic stem cell (HSC) self-renewal, demonstrating superior potency compared to p27 in mouse models. P18IN005 hydrochloride enhances the expansion of functional HSCs in short-term cultures, making it a valuable reagent for investigating the signaling pathways that govern stem cell self-renewal and differentiation processes.
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Cdc7-IN-17 is a potent inhibitor of CDC7, exhibiting an IC50 of less than 10 μM. This compound is designed for use in cancer research, particularly in studies focusing on cell cycle regulation and tumor progression. By targeting CDC7, Cdc7-IN-17 offers valuable insights into the mechanisms of cancer proliferation and potential therapeutic strategies.
CDK4/6-IN-14 is a potent and highly selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), displaying IC50 values of 10 nM and 16 nM, respectively. This compound exhibits over 60-fold selectivity compared to CDK1, CDK2, CDK7, and CDK9, while demonstrating high specificity against a broader panel of 205 kinases. CDK4/6-IN-14 is valuable for research into cell cycle regulation and has potential applications in studying cancer therapeutics and targeted therapies.
CDK9-IN-15 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), a key regulator of transcription elongation. By inhibiting CDK9, this compound effectively reduces the phosphorylation of RNA polymerase II, leading to decreased transcriptional activity of oncogenes. CDK9-IN-15 is primarily utilized in cancer research to explore therapeutic strategies that target transcriptional regulation in malignancies.
CDK7-IN-13 is a potent inhibitor of cyclin-dependent kinase 7 (CDK7), with a pyrimidinyl derivative structure. This compound exhibits significant activity against cancer cells characterized by transcriptional dysregulation, making it a valuable tool for cancer research. Its application in studies targeting CDK7 may enhance the understanding of cancer biology and aid in the development of novel therapeutic strategies.
CDK9-IN-48 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), demonstrating an IC50 value of 1.37 nM. This compound effectively suppresses the proliferation of a variety of cancer cell lines, making it a valuable tool in cancer research. CDK9-IN-48 is particularly relevant for studies focused on acute myeloid leukemia and prostate cancer, where targeting CDK9 may provide therapeutic benefits.
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CDK12/13-IN-1 is a selective inhibitor of cyclin-dependent kinases 12 and 13 (CDK12/13). This compound demonstrates significant antitumor activity by interfering with the phosphorylation of RNA polymerase II, thereby disrupting transcriptional regulation in cancer cells. CDK12/13-IN-1 is utilized in research focused on cancer biology, particularly in exploring therapeutic strategies for tumors exhibiting CDK12/13 dependency.
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Synonyms: SHR-6390 isethionate
Dalpiciclib isethionate is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). By inhibiting the kinase activity of these enzymes, Dalpiciclib effectively disrupts the progression of the cell cycle from the G1 phase to the S phase, which reduces abnormal cellular proliferation. This compound is primarily utilized in cancer research, particularly in the study of breast cancer, where CDK4/6 dysregulation plays a critical role in tumor growth.
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CDK-IN-10 is a potent cyclin-dependent kinase (CDK) inhibitor that selectively blocks CDK activity. This compound has demonstrated significant antitumor effects, making it an invaluable tool for cancer research. Researchers can utilize CDK-IN-10 to investigate CDK regulation in cell cycle progression and explore its potential in therapeutic applications against various cancers.
CDK8-IN-10 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), exhibiting an IC50 value of 8.25 nM. This compound is instrumental in the study of CDK8's role in cancer progression and may provide insights into therapeutic strategies targeting this kinase. Its potency and selectivity make it a valuable tool for cancer research applications.
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