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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.
CDK9-IN-38 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting IC50 values of 1.2 nM for the wild-type enzyme and 3.3 nM for the L156F mutant variant. This compound has demonstrated significant inhibitory effects on tumor growth in both in vitro and in vivo models. CDK9-IN-38 is a valuable tool for research into the regulation of transcriptional control and the therapeutic potential for cancer treatment.
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CDK4/6-IN-7 is a potent and selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), with IC50 values of 1.58 nM and 4.09 nM, respectively. This orally active compound demonstrates significant biological activity, making it a valuable tool for investigating the role of CDK4/6 in various cancer models, particularly in breast cancer research. Its specificity and efficacy support studies aimed at understanding and targeting cell cycle progression in tumor cells.
Cdc7-IN-15 is a selective inhibitor of Cdc7 kinase, a crucial regulator of the cell cycle. This compound exhibits significant anti-proliferative activity, making it a valuable tool for cancer research. It is particularly useful for studies investigating the role of Cdc7 in tumorigenesis and as a potential therapeutic target in cancer treatment.
PF-06842874 is a selective inhibitor of CDK4 and CDK6, targeting the cyclin D1 and cyclin D3 complexes with Ki values of 62 nM and 130 nM, respectively. This compound demonstrates significant biological activity in the inhibition of cell proliferation, making it a valuable tool in cancer research and the study of pulmonary arterial hypertension. Its ability to modulate cell cycle progression positions PF-06842874 as an important reagent for investigating therapeutic strategies in oncological and vascular disease contexts.
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CDK7-IN-32 is a potent inhibitor of Cyclin-dependent kinase 7 (CDK7), a key regulator of cell cycle progression and transcriptional regulation. This compound effectively disrupts CDK7 activity, leading to decreased phosphorylation of its substrates and subsequent modulation of cellular proliferation and survival. CDK7-IN-32 is utilized in cancer research and studies investigating the role of CDK7 in transcriptional control and therapeutic resistance.
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CDK9-IN-28 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), which plays a critical role in regulating transcription and cell cycle progression. This compound exhibits strong anti-proliferative effects, particularly in solid tumor models, making it valuable for cancer research. Additionally, CDK9-IN-28 serves as a target protein ligand for the synthesis of PROTACs, aiding in the development of innovative therapeutic strategies for targeting CDK9-dependent pathways.
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LZ9 is an ATP-competitive inhibitor of CDK1 and CDK2. This compound demonstrates significant biological activity in inhibiting cyclin-dependent kinases, making it a valuable tool for investigating cell cycle regulation. LZ9 has potential applications in research focused on colorectal cancer (CRC), aiding in the exploration of therapeutic strategies targeting this malignancy.
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CDK9-IN-49 is a potent inhibitor of Cyclin-dependent kinase 9 (CDK9) with an IC50 of 7.32 nM. This compound effectively suppresses the proliferation of various cancer cell lines, making it a valuable tool for cancer research. CDK9-IN-49 is particularly relevant for studies focused on acute myeloid leukemia and prostate cancer, facilitating investigations into therapeutic strategies targeting CDK9 pathways.
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CDK4/6-IN-24 is a potent inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), key regulators of the cell cycle. This compound demonstrates broad-spectrum antitumor activity across various cancer cell lines, with IC50 values in the submicromolar range. CDK4/6-IN-24 is a valuable tool for researchers investigating cell cycle regulation and therapeutic strategies for cancer treatment.
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CDK2-IN-54 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), a critical regulator of the cell cycle. This compound demonstrates potent anti-proliferative activity in various cancer types, including triple-negative breast cancer, ovarian cancer, bladder cancer, and uterine cancer. CDK2-IN-54 is valuable for research applications focused on understanding cell cycle dynamics and exploring therapeutic strategies in oncology.
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CDK4/6-IN-21 maleate is a potent inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), exhibiting IC50 values of 3.88 nM and 3.31 nM against CDK4 and CDK6, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for research into cell cycle regulation and cancer therapeutics. Its targeted inhibition of CDK4/6 positions it as a key reagent for studying oncogenic pathways and developing new cancer treatment strategies.
CDK4/6-IN-20 is a potent inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/CDK6), demonstrating IC50 values of 1.9 nM and 14.2 nM, respectively. This compound effectively inhibits cell proliferation, making it a valuable tool for cancer research applications. Its selective inhibition of CDK4/6 contributes to understanding cell cycle regulation and potential therapeutic interventions in malignancies.
CGP-79807 is a purine-based inhibitor targeting cyclin-dependent kinases (CDKs). It effectively disrupts the cell cycle by inhibiting CDK activity, leading to the suppression of tumor cell proliferation. This compound is valuable in cancer research for exploring the mechanisms of cell cycle regulation and potential therapeutic strategies.
CDK2/4/6-IN-1 is a potent inhibitor of cyclin-dependent kinases 2, 4, and 6, with IC50 values of 2.5 nM, 23.7 nM, and 44.3 nM, respectively. This compound is valuable for cancer research, allowing for the study of cell cycle regulation and tumor progression. Additionally, CDK2/4/6-IN-1 features an alkyne group enabling its use in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, facilitating bioconjugation and labeling applications in chemical biology.
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CDK7-IN-22 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7) with demonstrated antitumor activity. Its inhibition of CDK7 plays a crucial role in modulating transcriptional regulation and cell cycle progression, making it a valuable tool for cancer research. CDK7-IN-22 is suitable for studies on tumorigenesis, therapeutic resistance, and cellular proliferation pathways.
CDK7-IN-14 is a selective inhibitor of cyclin-dependent kinase 7 (CDK7), a key enzyme involved in transcriptional regulation and cell cycle progression. This pyrimidinyl derivative exhibits significant potential in cancer research, particularly in the study of tumors characterized by transcriptional dysregulation. CDK7-IN-14 may serve as a valuable tool for investigating therapeutic strategies targeting CDK7 in various malignancies.
Synonyms: (+)-BAY-1143572; d-BAY-1143572
(+)-Atuveciclib is a selective inhibitor of cyclin-dependent kinase 9 (CDK9) and the positive transcription elongation factor b (P-TEFb). With an IC50 value of 13 nM, it effectively suppresses CDK9 in cellular assays. This compound is primarily utilized in research related to transcription regulation and cancer therapeutics, offering insights into CDK9-mediated pathways and their role in various malignancies.
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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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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.
